Ph.D from UDCT, now ICT, Mumbai,INDIA, In Organic Chemistry, under Prof. S. SESHADRI, 25+ years in industry( API), mostly multinationals, Conducted process development in companies like Hoechst Marion Roussel(Sanofi aventis), Searle, Schering, RPG, Innovassynth, Glenmark, with exposure to basic research at SEARLE under Dr Nagarajan (Director Ciba), Tech transfer in plant eg deltamethrin 3 tonnes in RPG, bulk drug gmp (only 7 months) in Hoechst Marion Roussel(SANOFI AVENTIS), Custom synthesis in Innovasynth(SANDOZ, Basel, BASF Germany), exposure to Natural products, drugs intermediates, vet drugs, and some exposure in agro.speciality chemicals, flavours and fragrances, nutraceuticals and mettalocenes. ability to deliver products in the production plant(atleast 35 in career).Helping millions with websites on chemistry, million hits on google


1. Felt proud to spend millenium night in plant for deltamethrin

2. Added personally a 25 kg sodium cyanide charge in a reactor at 2.oo in night, panoli, gujarat, India at 90'decade, not to be attempted again

3. Did not run away and controlled an exotherm in plant batch due to accidental addn of acid.Chloridel into NaCN rxn , the batch was to be done at zero degrees cent and temp went upto 61 degrees cent

4. Similar case when a thin film high vac distn exploded in a pilot plant in nasik for CBZ chem. UK, still able to despatch 100 kg material, Award london trip

5. High vac. distilled 25 kg of drug int in the night using 3 pumps for a pilot plant trial intermediate, SANDOZ Basel Customer, award bottle of wine from switzerland

6. Personally worked after lab work in evenings with Dr Ralph Stapel , director. in modern, Hoechst pilot plant at Mulund Mumbai, in 80'

7. Assisted Head Asia pacific, QA for TGA audit at Aventis plant ankleshwar

8 Slept for 3 hrs in morning in first aid room in Panoli during deltamethrin process demo at panoli Gujarat, then afternoon 2 hrs at guest house during 6 months campaign, Walked to ankleshwar 10 km in night on non availability if transport

9 Reached Innovasynth lab in khopoli at 9 morning from mumbai,100 km, using trucks, ricks after july monsoon deluge in Mumbai 2005

10 Got an opportunity to write a DMF in 90', Hoechst, Got a chance to work in departments like tablets,large vol parenterals, injections, vaccines , liq orals, enzymes in Hoechst mulund, mumbai, India plant


11 Most crazy thing was to add 3 litres of butyl lithium solution by gravity using a cannula by carrying it on my shoulder



To carry out research and devpt, motivate, guide & lead a team of scientists,conduct,identify and execute new/novel routes for the synth,scale up from grams to kg levels in lab,conduct pilot trials/assist in prodn.upto ton levels. Carry out impurity profiles and assist in dossier writing. To keep in mind IPR issues and draft patents, file DMFS in US/EU, file patents and contribute to intellectual property,Ability to develop novel routes for API,s, well versed with polymorphism issues



molecules reacting


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    konteyner fiyatları (Thursday, 01 August 2013 10:28)

    ve gitti. taşımacılığı <br />uzun ve kaba ve neredeyse kıyıdan için, bir koltukta yatıyordu ebatları <br />bu, önlem ve form meselesi olarak, gerekli görülen lojistik <br />bu, onun çıkarıldıktan sonra kafasına mücadele olmamış onun jdownloader





Sreeni Labs Private Limited, Hyderabad, India ready to deliver New, Economical, Scalable Routes in your early Clinical Drug Development Stages

str1   Sreeni Labs Private Limited, Hyderabad, India is ready to take up challenging synthesis projects from your preclinical and clinical development and supply from few grams to multi-kilo quantities. Sreeni Labs has proven route scouting ability  to  design and develop innovative, cost effective, scalable routes by using readily available and inexpensive starting materials. The selected route will be further developed into a robust process and demonstrate on kilo gram scale and produce 100's of kilos of in a relatively short time. Accelerate your early development at competitive price by taking your route selection, process development and material supply challenges (gram scale to kilogram scale) to Sreeni Labs…………


Sreeni Labs based in Hyderabad, India is working with various global customers and solving variety of challenging synthesis problems. Their customer base ranges from USA, Canada, India and Europe. Sreeni labs Managing Director, Dr. Sreenivasa Reddy Mundla has worked at Procter & Gamble Pharmaceuticals and Eli Lilly based in USA. The main strength of Sreeni Labs is in the design, development of innovative and highly economical synthetic routes and development of a selected route into a robust process followed by production of quality product from 100 grams to 100s of kg scale. Sreeni Labs main motto is adding value in everything they do. They have helped number of customers from virtual biotech, big pharma, specialty chemicals, catalog companies, and academic researchers and drug developers, solar energy researchers at universities and institutions by successfully developing highly economical and simple chemistry routes to number of products that were made either by very lengthy synthetic routes or  by using highly dangerous reagents and Suzuki coupling steps. They are able to supply materials from gram scale to multi kilo scale in a relatively short time by developing very short and efficient synthetic routes to a number of advanced intermediates, specialty chemicals, APIs and reference compounds. They also helped customers by drastically reducing number of steps, telescoping few steps into a single pot. For some projects, Sreeni Labs was able to develop simple chemistry and avoided use of palladium & expensive ligands. They always begin the project with end in the mind and design simple chemistry and also use readily available or easy to prepare starting materials in their design of synthetic routes Over the years, Sreeni labs has successfully made a variety of products ranging from few mg to several kilogram scale. Sreeni labs has plenty of experience in making small select libraries of compounds, carbocyclic compounds like complex terpenoids, retinal derivatives, alkaloids, and heterocyclic compounds like multi substituted beta carbolines, pyridines, quinolines, quinolones, imidazoles, aminoimidazoles, quinoxalines, indoles, benzimidazoles, thiazoles, oxazoles, isoxazoles, carbazoles, benzothiazoles, azapines, benzazpines, natural and unnatural aminoacids, tetrapeptides, substituted oligomers of thiophenes and fused thiophenes, RAFT reagents, isocyanates, variety of ligands,  heteroaryl, biaryl, triaryl compounds, process impurities and metabolites. Sreeni Labs is Looking for any potential opportunities where people need development of cost effective scalable routes followed by quick scale up to produce quality products in the pharmaceutical & specialty chemicals area. They can also take up custom synthesis and scale up of medchem analogues and building blocks.  They have flexible business model that will be in sink with customers. One can test their abilities & capabilities by giving couple of PO based (fee for service) projects.     See presentation below LINK ON SLIDESHARE Managing Director at Sreeni Labs Private Limited The man behind Seeni labs is Dr. Sreenivasa Mundla Reddy Sreenivasa Reddy

Dr. Sreenivasa Reddy Mundla

Managing Director at Sreeni Labs Private Limited Sreeni Labs Private Limited Road No:12, Plot No:24,25,26
  • IDA, Nacharam Hyderabad, 500076 Telangana State, India


LINKEDIN FACEBOOK RESEARCHGATE EMAIL,, Dr. Sreenivasa Mundla Reddy Dr. M. Sreenivasa Reddy obtained Ph.D from University of Hyderabad under the direction Prof Professor Goverdhan Mehta in 1992. From 1992-1994, he was a post doctoral fellow at University of Wisconsin in Professor Jame Cook's lab. From 1994 to 2000,  worked at Chemical process R&D at Procter & Gamble Pharmaceuticals (P&G). From 2001 to 2007 worked at Global Chemical Process R&D at Eli Lilly and Company in Indianapolis.  In 2007  resigned to his  job and founded Sreeni Labs based in Hyderabad, Telangana, India  and started working with various global customers and solving various challenging synthesis problems.  The main strength of Sreeni Labs is in the design, development of a novel chemical route and its development into a robust process followed by production of quality product from 100 grams to 100's of kg scale. 
They have helped number of customers by successfully developing highly economical simple chemistry routes to number of products that were made by Suzuki coupling. they are able to shorten the route by drastically reducing number of steps, avoiding use of palladium & expensive ligands. they always use readily available or easy to prepare starting materials in their design of synthetic routes.
Sreeni Labs is Looking for any potential opportunities where people need development of cost effective scalable routes followed by quick scale up to produce quality products in the pharmaceutical & specialty chemicals area. They have flexible business model that will be in sink with customers. One can test their abilities & capabilities by giving PO based projects


Founder & Managing Director

Sreeni Labs Private Limited
August 2007 – Present (8 years 11 months)
Sreeni Labs Profile
Sreeni Labs Profile
View On SlideShare

Principal Research Scientist

Eli Lilly and Company
March 2001 – August 2007 (6 years 6 months)

Senior Research Scientist

Procter & Gamble
July 1994 – February 2001 (6 years 8 months)


University of Hyderabad

Doctor of Philosophy (Ph.D.), 
1986 – 1992
  PUBLICATIONS Article: Expansion of First-in-Class Drug Candidates That Sequester Toxic All-Trans-Retinal and Prevent Light-Induced Retinal Degeneration Jianye Zhang · Zhiqian Dong · Sreenivasa Reddy Mundla · X Eric Hu · William Seibel ·Ruben Papoian · Krzysztof Palczewski · Marcin Golczak Article: ChemInform Abstract: Regioselective Synthesis of 4Halo ortho-Dinitrobenzene Derivative Sreenivasa Mundla Aug 2010 · ChemInform Article: Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent Hong-yu Li · William T. McMillen · Charles R. Heap · Denis J. McCann · Lei Yan · Robert M. Campbell · Sreenivasa R. Mundla · Chi-Hsin R. King · Elizabeth A. Dierks · Bryan D. Anderson · Karen S. Britt · Karen L. Huss Apr 2008 · Journal of Medicinal Chemistry Article: ChemInform Abstract: A Concise Synthesis of Quinazolinone TGF-β RI Inhibitor Through One-Pot Three-Component Suzuki—Miyaura/Etherification and Imidate—Amide Rearrangement Reactions Hong-yu Li · Yan Wang · William T. McMillen · Arindam Chatterjee · John E. Toth ·Sreenivasa R. Mundla · Matthew Voss · Robert D. Boyer · J. Scott Sawyer Feb 2008 · ChemInform Article: ChemInform Abstract: A Concise Synthesis of Quinazolinone TGF-β RI Inhibitor Through One-Pot Three-Component Suzuki—Miyaura/Etherification and Imidate—Amide Rearrangement Reactions Hong-yu Li · Yan Wang · William T. McMillen · Arindam Chatterjee · John E. Toth ·Sreenivasa R. Mundla · Matthew Voss · Robert D. Boyer · J. Scott Sawyer Nov 2007 · Tetrahedron Article: Dihydropyrrolopyrazole Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: A Novel Benzimidazole Series with Selectivity versus Transforming Growth Factor-β Type II Receptor Kinase and Mixed Lineage Kinase-7 Hong-yu Li · Yan Wang · Charles R Heap · Chi-Hsin R King · Sreenivasa R Mundla · Matthew Voss · David K Clawson · Lei Yan · Robert M Campbell · Bryan D Anderson · Jill R Wagner ·Karen Britt · Ku X Lu · William T McMillen · Jonathan M Yingling Apr 2006 · Journal of Medicinal Chemistry Read full-textSource Article: Studies on the Rh and Ir mediated tandem Pauson–Khand reaction. A new entry into the dicyclopenta[ a, d]cyclooctene ring system Hui Cao · Sreenivasa R. Mundla · James M. Cook Aug 2003 · Tetrahedron Letters Article: ChemInform Abstract: A New Method for the Synthesis of 2,6-Dinitro and 2Halo6-nitrostyrenes Sreenivasa R. Mundla Nov 2000 · ChemInform Article: ChemInform Abstract: A Novel Method for the Efficient Synthesis of 2-Arylamino-2-imidazolines

Read at


Patents by Inventor Dr. Sreenivasa Reddy Mundla
  • Patent number: 7872020
    Abstract: The present invention provides crystalline 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro -4H-pyrrolo[1,2-b]pyrazole monohydrate.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: January 18, 2011
    Assignee: Eli Lilly and Company
    Inventor: Sreenivasa Reddy Mundla
  • Publication number: 20100120854
    Abstract: The present invention provides crystalline 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate.
    Type: Application
    Filed: June 29, 2006
    Publication date: May 13, 2010
    Inventor: Sreenivasa Reddy Mundla
  • Patent number: 6066740
    Abstract: The present invention provides a process for making 2-amino-2-imidazoline, guanidine, and 2-amino-3,4,5,6-tetrahydroyrimidine derivatives by preparing the corresponding activated 2-thio-subsituted-2-derivative in a two-step, one-pot procedure and by further reacting yields this isolated derivative with the appropriate amine or its salts in the presence of a proton source. The present process allows for the preparation of 2-amino-2-imidazolines, quanidines, and 2-amino-3,4,5,6-tetrahydropyrimidines under reaction conditions that eliminate the need for lengthy, costly, or multiple low yielding steps, and highly toxic reactants. This process allows for improved yields and product purity and provides additional synthetic flexibility.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: May 23, 2000
    Assignee: The Procter & Gamble Company
    Inventors: Michael Selden Godlewski, Sean Rees Klopfenstein, Sreenivasa Reddy Mundla, William Lee Seibel, Randy Stuart Muth
TGF-β inhibitors US 7872020 B2
Sreenivasa Reddy Mundla The present invention provides 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl) -5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole monohydrate, i.e., Formula I.
Figure US07872020-20110118-C00002
EXAMPLE 1 Preparation of 2-(6-methyl-pyridin-2-yl)-3-[6-amido-quinolin-4-yl-5,6-dihydro-4H -pyrrolo[1,2-b]pyrazole monohydrate
Figure US07872020-20110118-C00008
Galunisertib 1H NMR (CDCl3): δ=9.0 ppm (d, 4.4 Hz, 1H); 8.23-8.19 ppm (m, 2H); 8.315 ppm (dd, 1.9 Hz, 8.9 Hz, 1H); 7.455 ppm (d, 4.4 Hz, 1H); 7.364 ppm (t, 7.7 Hz, 1H); 7.086 ppm (d, 8.0 Hz, 1H); 6.969 ppm (d, 7.7 Hz, 1H); 6.022 ppm (m, 1H); 5.497 ppm (m, 1H); 4.419 ppm (t, 7.3 Hz, 2H); 2.999 ppm (m, 2H); 2.770 ppm (p, 7.2 Hz, 7.4 Hz, 2H); 2.306 ppm (s, 3H); 1.817 ppm (m, 2H). MS ES+: 370.2; Exact: 369.16 ABOVE MOLECULE IS
Phase III
CAS No.700874-72-2
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KEYWORDS   Sreenivasa Mundla Reddy, Managing Director, Sreeni Labs Private Limited, Hyderabad, Telangana, India,  new, economical, scalable routes, early clinical drug development stages, Custom synthesis, custom manufacturing, drug discovery, PHASE 1, PHASE 2, PHASE 3,  API, drugs, medicines





ENDO EXO STORY.......cis-norborene-5,6-endo-dicarboxylic anhydride


You will react cyclopentadiene with maleic anhydride to form the Diels-Alder product below. This Diels-Alder reaction produces almost solely the endo isomer upon reaction at ambient temperature.


The preference for endo–stereochemistry is “observed” in most Diels-Alder reactions. The fact that the more hindered endo product is formed puzzled scientists until Woodward, Hoffmann, and Fukui used molecular orbital theory to explain that overlap of the p orbitals on the substituents on the dienophile with p orbitals on the diene is favorable, helping to bring the two molecules together.

Hoffmann and Fukui shared the 1981 Nobel Prize in chemistry for their molecular orbital explanation of this and other organic reactions. In the illustration below, notice the favorable overlap (matching light or dark lobes) of the diene and the substituent on the dienophile in the formation of the endo product:


Oftentimes, even though the endo product is formed initially, an exo isomer will be isolated from a Diels-Alder reaction. This occurs because the exo isomer, having less steric strain than the Endo , is more stable, and because the Diels-Alder reaction is often reversible under the reaction conditions. In a reversible reaction, the product is formed, reverts to starting material, and forms again many times before being isolated.

The more stable the product, the less likely it will be to revert to the starting material. The isolation of an exo product from a Diels-Alder reaction is an example of an important concept: thermodynamic vs kinetic control of product composition. The first formed product in a reaction is called the kinetic product. If the reaction is not reversible under the conditions used, the kinetic product will be isolated. However, if the first formed product is not the most stable product and the reaction is reversible under the conditions used, then the most stable product, called the thermodynamic product, will often be isolated.

The NMR spectrum of cis-5-norbornene-2,3-endo-dicarboxylic anhydride is given below:

Cis-Norbornene-5,6-endo-dicarboxylic anhydride 
Cyclopentadiene was previously prepared through the cracking of dicyclopentadiene and kept under cold conditions.  In a 25 mL Erlenmeyer flask, maleic anhydride (1.02 g, 10.4 mmol) and ethyl acetate (4.0 mL) were combined, swirled, and slightly heated until completely dissolved.  To the mixture, ligroin (4 mL) was added and mixed thoroughly until dissolved.  Finally, cyclopentadiene (1 mL, 11.9 mmol) was added to the mixture and mixed extensively.  The reaction was cooled to room temperature and placed into an ice bath until crystallized.  The crystals were isolated through filtration in a Hirsch funnel.  The product had the following properties: 0.47 g (27.6% yield) mp: 163-164 °C (lit: 164 °C).  1H NMR (CDCl3, 300 MHz) δ: 6.30 (dd, J=1.8 Hz, 2H), 3.57 (dd, J=7.0 Hz, 2H), 3.45 (m, 2H), 1.78 (dt, J=9.0,1.8 Hz, 1H), 1.59 (m, 1H) ppm.  13C NMR (CDCl3, 75Hz) δ: 171.3, 135.5, 52.7, 47.1, 46.1 ppm.  IR 2982 (m), 1840 (s), 1767 (s), 1089 (m) cm-1.

Reaction Mechanism The scheme below depicts the concerted mechanism of the Diels-Alder reaction of cyclopentadiene and maleic anhydride to formcis-Norbornene-5,6-endo-dicarboxylic anhydride.

diels-alder reaction


Results and Discussion 
When combining the reagents, a cloudy mixture was produced and problems arose in the attempt to completely dissolve the mixture.  After heating for about 10 minutes and magnetically stirring, tiny solids still remained. The undissolved solids were removed form the hot solution by filtration and once they cooled, white crystals began to form. Regarding the specific reaction between cyclopentadiene and maleic anhydride, the endo isomer, the kinetic product, was formed because the experiment was directed under mild conditions.   The exo isomer is the thermodynamic product because it is more stable.3
A total of 0.47 g of the product was collected; a yield of 27.6%. The melting point was in the range of 163-164 °C which indicates the absence of impurities because the known melting point of the product is 164 °C.
Cis-Norbornene-5-6-endo-dicarboxylic anhydride

The 1H NMR spectrum of the product revealed a peak in the alkene range at 6.30 ppm, H-2 and H-3 (Figure 1).  In addition, it exhibited two peaks at 3.57 and 3.45 ppm because of the proximity of H-1, H-4, H-5, and H-6 to an electronegative atom, oxygen.  Finally, two peaks at 1.78 and 1.59 ppm corresponded to the sp3 hydrogens, Hb and Ha, respectively.  Impurities that appeared included ethyl acetate at 4.03, 2.03, and 1.31 ppm as well as acetone at 2.16 ppm.
Regarding the 13C NMR, a peak appeared at 171.3 ppm, accounting for the presence of two carbonyl functional groups, represented by C-7 and C-8 in Figure 1.  The alkene carbons, C-2 and C-3, exhibited a peak at 135.5 ppm, while the sp3 carbons close to oxygen, C-5 and C-6, displayed a peak at 52.7 ppm.  Finally, peaks at 46.1 and 47.1 ppm accounted for the sp3 carbons, C-1 and C-4, and C-9.  Impurities of ethyl acetate appeared at 46.6, 25.8, and 21.0 ppm accompanied with acetone at 30.9 ppm.
The IR spectrum revealed a peak at 2982 cm-1 representing the C-H stretches.  A peak at 1840 cm-1 accounted for the carbonyl functional group, while a peak at 1767 cm-1 accounted for the alkene bond.  A peak at 1089 cm-1 represented the carbon-oxygen functional group.
In order to distinguish between the two possible isomers, properties such as melting point and spectroscopy data were analyzed.  The exo product possessed a melting point in the range of 140-145 °C which is significantly lower than the endo product.  The observed melting point in this experiment supported the production of the endo isomer. 
The 1H NMR spectum exhibited a doublet of doublets at 3.57 ppm for the endo isomer.  The exo isomer would possess a triplet around 3.50 ppm due to the difference in dihedral angle between the hydrogen molecules of H-1 and H-4, and H-5 and H-6 (Figure 1).  A peak at 3.00 ppm would appear in the exo isomer spectra as opposed to a peak at 3.60 ppm as shown in the observed endo product.3 This is because of the interaction and coupling with the H-5 and H-6, as displayed in Figure 1.
Through the Diels-Alder reaction, 27.6% yield of cis-Norbornene-5,6-endo-dicarboxylic anhydride was produced. The distinction of the presence of the endo isomer was proven by analyzing physical properties of both possible isomers.
Martin, J.; Hill, R.; Chem Rev, 196161, 537-562.
2 Pavia, L; Lampman, G; Kriz, G; Engel, R. A Small Scale Approach to Organic Laboratory   Techniques, 2011, 400-409.
3 Myers, K.; Rosark, J. Diels-Alder Synthesis, 2004, 259-265.


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Iron-Catalyzed Oxidative Amidation of Tertiary Amines with Aldehydes

Thumbnail image of graphical abstract




 Iron-Catalyzed Oxidative Amidation of Tertiary Amines with Aldehydes (pages 82–86)

Yuanming Li, Fan Jia and Prof. Dr. Zhiping Li

Chemistry - A European Journal

Volume 19Issue 1pages 82–86January 2, 2013

Article first published online: 3 DEC 2012 | DOI: 10.1002/chem.201203824


Unconventional couple: A new oxidative coupling protocol for amide bond formation has been developed (see scheme). The method provides an efficient and practical route for the synthesis of tertiary amides from readily available tertiary amines and aldehydes in the presence of a simple FeCl2catalyst. Mechanistic studies indicated that a peroxide and an iminium ion act as the reactive intermediates in this oxidative amidation.


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One-Pot Synthesis of Alkyl Styryl Sulfides Free from Transition Metal/Ligand Catalyst and Thiols

Thumbnail image of graphical abstract One-Pot Synthesis of Alkyl Styryl Sulfides Free from Transition Metal/Ligand Catalyst and Thiols

European Journal of Organic Chemistry

Early View (Online Version of Record published before inclusion in an issue) Adrián A. Heredia and Alicia B. Peñéñory Article first published online: 19 DEC 2012 | DOI: 10.1002/ejoc.201201163 They have developed a one-pot methodology for the synthesis of alkyl arylvinyl sulfides in good to excellent yields, free of any metal/ligand systems and from malodorous and air-sensitive alkyl thiols. This procedure uses commercially available potassium thioacetate, low temperatures, and short reaction times.

abstract A new protocol for the one-pot synthesis of styryl alkyl sulfides was developed. This methodology involves the in situ generation of thiolate anions by nucleophilic substitution between potassium thioacetate and alkyl halides followed by fragmentation. Further reactions of these thiolate anions with substituted (E,Z)-β-styryl halides gave the corresponding sulfides with retention of stereochemistry in good to excellent yields. This procedure does not require a metal catalyst, it proceeds under mild conditions and in short times, and it is free from malodorous and air-sensitive alkyl thiols.   THANKS AND REGARD'S DR ANTHONY MELVIN CRASTO Ph.D MOBILE-+91 9323115463 GLENMARK SCIENTIST , NAVIMUMBAI, INDIA web link Congratulations! Your presentation titled "Anthony Crasto Glenmark scientist, helping millions with websites" has just crossed MILLION views.  アンソニー 安东尼 Энтони أنتوني  join my process development group on google 






The Formal Total Synthesis of FR252921 – An Immunosuppressant

Abstract Image The Formal Total Synthesis of FR252921 – An Immunosuppressant European Journal of Organic Chemistry Volume 2013, Issue 2, pages 376–388, January 2013 J. S. Yadav and Sandip Sengupta Article first published online: 15 NOV 2012 | DOI: 10.1002/ejoc.201201097 Related topics   The formal total synthesis of FR252921 is described. The key steps include the preparation of three fragments starting from 1,4-butanediol, (R)-malic acid, and prenol, respectively, followed by two consecutive peptide couplings of the three fragments. AbstractClick on the mini-structures! The formal total synthesis of FR252921 is described. The key steps include the preparation of three fragments starting from 1,4-butanediol, (R)-malic acid, and prenol, respectively, followed by two consecutive peptide couplings of the three fragments. Other key steps involve an allene-type rearrangement or enyne isomerization to install the triene moiety, a Seebach methylation, a Julia olefination to construct the trisubstituted diene unit, and an enzymatic resolution strategy to generate the C-18 stereocenter. other articles of relevance

J Antibiot (Tokyo). 2003 Feb;56(2):62-7.

FR252921, a novel immunosuppressive agent isolated from Pseudomonas fluorescens no. 408813 II. In vitro property and mode of action.

Fujine KAbe F, Seki N, Ueda H, Hino M, Fujii T.


Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2698, Japan.


A novel immunosuppressive agent, FR252921 was isolated from the cultured broth of a species of Pseudomonas fluorescens. We have shown that FR252921 inhibited splenic proliferation stimulated with LPS, insensitive to calcinuerin inhibitor. In this study, FR252921 was found to inhibit IL-2 and IL-12 production as well as proliferaion of splenocyte. Analysis of transcription activity revealed that FR252921 inhibited activating protein-1 (AP-1). Exposures of antigen presenting cells (APC) to FR252921 attenuated proliferation supplemented by naïve T cells. Further, FR252921 strongly suppressed splenic dendritic cell proliferation stimulated with LPS and anti-CD40 mAb, while it did not inhibit purified T cell activation, including CD154 expression and IL-2 production. These results suggest that APC is dominant target cell population.
Chemistry. 2009;15(14):3457-73. doi: 10.1002/chem.200802649.

Synthesis of two bioactive natural products: FR252921 and pseudotrienic acid B.

Amans D, Bellosta V, Cossy J.


Laboratoire de Chimie Organique, ESPCI ParisTech, CNRS, 10 rue Vauquelin, 75231 Paris, France.


Concise and highly convergent syntheses of the immunosuppressive agent FR252921 and the related antimicrobial natural product pseudotrienic acid B were achieved from a common intermediate by using optically active titanium complexes to control the configuration of the stereogenic centers, a highly stereo- and regioselective cross-metathesis to generate the triene moieties, and a Stille cross-coupling to install the dienic units.

Synthesis of a Promising Immunosuppressant:  FR252921

Dominique Amans , Véronique Bellosta , and Janine Cossy
Laboratoire de Chimie Organique, ESPCI, CNRS, 10 rue Vauquelin, 75231 Paris Cedex 05, France
Org. Lett., 2007, 9 (23), pp 4761–4764
DOI: 10.1021/ol702110k
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The α-tocopherol form of vitamin E Vitamin E refers to a group of eight fat-soluble compounds that include both tocopherolsand tocotrienols.[1] There are many different forms of vitamin E, of which γ-tocopherol is the most common in the North American diet.[2] γ-Tocopherol can be found in corn oil, soybean oil, margarine and dressings.[3][4] In the North American diet, α-Tocopherol, the most biologically active form of vitamin E, is the second most common form of vitamin E. This variant of vitamin E can be found most abundantly in wheat germ oil, sunflower, and safflower oils.[4][5] It is a fat-soluble antioxidant that stops the production of reactive oxygen species formed when fat undergoes oxidation.[6][7][8]

  • Synthesis of Vitamin E

Vitamin E (CAS NO.: 59-02-9), with other names as 2(R),5,7,8-Tetramethyl-2-[4(R),8(R),12-trimethyltridecyl]-3,4-dihydro-2H-1-benzopyran-6-ol, could be produced through the following synthetic routes.Dictionary,

 Synthesis of Vitamin E
           Synthesis of Vitamin E
The chlorination of myrcene (I) with Cl2 in refluxing pentane gives the choromyrcene (II), and the hydrochlorination of (I) catalyzed by CuCl yields a mixture of geranyl/neryl chloride (III). The reductive coupling of (II) and (III) by means of Mg and CuCl affords beta-springene (IV), which is condensed with 2,3,6-trimethylhydroquinone (V) by means of cyclooctadienyl rhodium chloride dimer [RhCl(COD)]2 and K2CO3 in refluxing toluene to provide the adduct (VI). The cyclization of (VI) by means of MeAlCl2 of Ts-OH in refluxing hexane furnishes the tocotrienol (VII), which is finally hydrogenated with H2 over Pd/C in ethanol to give the target (rac)-vitamin E.


  1. Brigelius-Flohe, B; Traber (1999). "Vitamin E: function and metabolism". FASEB 13: 1145–1155.
  2. Traber, MG (1998). "The biological activity of vitamin E". The Linus Pauling Institute. Retrieved 6 March 2011.
  3. Bieri, JG; Evarts (1974). "γ-Tocopherol: metabolism, biological activity and significance in human vitamin E nutrition". American Journal of Clinical Nutrition 27 (9): 980–986. PMID 4472121.
  4. Brigelius-Flohé R, Traber MG (1 July 1999). "Vitamin E: function and metabolism". FASEB J. 13 (10): 1145–55. PMID 10385606.
  5. Reboul E, Richelle M, Perrot E, Desmoulins-Malezet C, Pirisi V, Borel P (15 November 2006). "Bioaccessibility of carotenoids and vitamin E from their main dietary sources". Journal of Agricultural and Food Chemistry 54 (23): 8749–8755. doi:10.1021/jf061818s.PMID 17090117.
  6. National Institute of Health (4 May 2009). "Vitamin E fact sheet".
  7. Herrera; Barbas, C (2001). "Vitamin E: action, metabolism and perspectives". Journal of Physiology and Biochemistry 57 (2): 43–56.doi:10.1007/BF03179812PMID 11579997.
  8. Packer L, Weber SU, Rimbach G (2001). "Molecular aspects of α-tocotrienol antioxidant action and cell signalling"Journal of Nutrition 131 (2): 369S–73S. PMID 11160563.






Sulforaphane, a natural product present in cruciferous vegetables like broccoli, reduces childhood leukemia progression

Sulforaphane is a molecule, ref1 within the isothiocyanate group of organosulfur compounds. It exhibits anti-cancer and antimicrobial properties in experimental models. It is obtained from cruciferous vegetables such as broccoliBrussels sprouts or cabbages. It is produced when the enzyme myrosinase transforms glucoraphanin, a glucosinolate, into sulforaphane upon damage to the plant (such as from chewing) which allows the two compounds to mix and react. Young sprouts of broccoli and cauliflower are particularly rich in glucoraphanin.
glucoraphanin, glucosinolate precursor to sulforaphane
Sulforaphane, discovered by accident in 1995 by a group of scientists researching the anticancer compounds in broccoli, is a phytochemical compound that can be obtained by eating cruciferous vegetables such as arugula, watercress, Brussels sprouts, broccoli, broccoli sprouts, cabbage, cauliflower, bok choy, kale, collards, kohlrabi, mustard, turnip, radish and rutabaga.  Sulforaphane is particularly abundant in watercress and broccoli sprouts.

Sulforaphane, a natural product present in cruciferous vegetables like broccoli, reduces childhood leukemia progression

Sulforaphane Induces Cell Cycle Arrest and Apoptosis in Acute Lymphoblastic Leukemia Cells,
K. Suppipat, C. Shik Park, Y. Shen, X. Zhu, H. D. Lacorazza, 
PLOS ONE 2012.
DOI: 10.1371/journal.pone.0051251

 Related topics

click on above link

Sulforaphane is a phytochemical belonging to the family of isothiocyanates, which means it contains the typical NCS group.
Sulforaphane was identified in broccoli sprouts, which, of the cruciferous vegetables, have the highest concentration of sulforaphane. It is also found in Brussels sproutscabbage,cauliflowerbok choykalecollardsChinese broccolibroccoli raabkohlrabimustard,turnipradisharugula, and watercress
The optimal level of intake is not known, but some doctors recommend 200 to 400 mcg of sulforaphane daily from broccoli-sprout extracts.
Acute lymphoblastic leukemia is the most common form of blood cancer affecting children. Although the current treatments cure 8 % of the patients, in the remaining cases the disease recurs and it can be fatal. Thus, novel drugs effective against relapses are needed.

To this regard, Koramit Suppipat, Texas Children’s Hospital, USA, and colleagues investigated the anti leukemic properties of sulforaphane, a dietary isothiocyanate abundant in cruciferous vegetables, such as broccoli. This compound blocked the proliferation of pediatric leukemic cells and selectively promoted their death, mostly by inhibiting Akt and mTOR, two serine/threonine kinases necessary for the survival of these malignant cells. When administered orally to mice affected by leukemia, moreover, sulforaphane reduced the progression of the tumor.
This compound may thus be beneficial for acute lymphoblastic leukemia patients at high risk of relapse.
We know that stress accelerates aging and disease.  When you are under stress, your immune system is also compromised, weakening your ability to ward off invading organisms.  Chronic stress raises the level of the excitatory hormones, including norepinephrine and cortisol, which can wear your body down and lead to disease.  Sulforaphane inhibits the norepinephrine-mediated increase in the interleukin-6 levels in the cells, which is a very good thing.  Interleukin-6 is responsible for the shift from acute inflammation to chronic inflammation, the root of so many diseases.  Finding a safe and effective substance that can inhibit the overproduction of norepinephrine, like sulforaphane,  is a significant accomplishment.
Consumption of broccoli sprouts has shown to be potentially effective at inhibitingHelicobacter pylori growth,[2][3] with sulforaphane being at least one of the active agents.[4][2]
Sulforaphane and dietary consumption of cruciferous vegetables are known to affect the action of drug-metabolizing enzymes in vitroand in preliminary human studies.[5] Although no side effects or direct drug interactions have been reported as of 2008, people taking prescription drugs are advised to consult a doctor before taking sulforaphane or broccoli-sprout extracts.
The possible anticancer activity of sulforaphane may be related to the induction of phase-II enzymes of xenobiotic transformation (such as quinone reductase and glutathione S-transferase), and enhancing the transcription of tumor suppressor proteins, possibly via inhibitory effects on histone deacetylase.[6]
Sulforaphane and diindolylmethane (another compound from Brassica vegetables) inhibit cancer growth in vitro and in experimental animals.[7] Sulforaphane downregulated the Wnt/beta-catenin self-renewal pathway in breast cancer stem cells.[7]



MW: 177
Formula: C6H11NOS2


  1. Zhang Y, Talalay P, Cho CG, Posner GH (March 1992). "A major inducer of anticarcinogenic protective enzymes from broccoli: isolation and elucidation of structure"Proc. Natl. Acad. Sci. U.S.A. 89 (6): 2399–2403. doi:10.1073/pnas.89.6.2399PMC 48665.PMID 1549603.
  2. Yanaka A, Fahey JW, Fukumoto A, Nakayama M, Inoue S, Zhang S, Tauchi M, Suzuki H, Hyodo I, Yamamoto M (April 2009). "Dietary sulforaphane-rich broccoli sprouts reduce colonization and attenuate gastritis in Helicobacter pylori–infected mice and humans". Cancer Prev. Res. 2 (4): 353–360. doi:10.1158/1940-6207.CAPR-08-0192PMID 19349290Lay summary.
  3. Galan MV, Kishan AA, Silverman AL (August 2004). "Oral broccoli sprouts for the treatment of Helicobacter pylori infection: a preliminary report". Dig Dis Sci. 49 (7–8): 1088–1090. doi:10.1023/B:DDAS.0000037792.04787.8aPMID 15387326.
  4. Fahey JW, Haristoy X, Dolan PM et al. (May 2002). "Sulforaphane inhibits extracellular, intracellular, and antibiotic-resistant strains of Helicobacter pylori and prevents benzo[a]pyrene-induced stomach tumors"Proc. Natl. Acad. Sci. U.S.A. 99 (11): 7610–7615.doi:10.1073/pnas.112203099PMC 124299PMID 12032331.
  5. Kall MA, Vang O, Clausen J (March 1997). "Effects of dietary broccoli on human drug metabolising activity". Cancer Lett. 114 (1–2): 169–170. doi:10.1016/S0304-3835(97)04652-1PMID 9103281.
  6. Hayes, JD; Kelleher, MO; Eggleston, IM (2008). "The cancer chemopreventive actions of phytochemicals derived from glucosinolates".European Journal of Nutrition 47 Suppl 2: 73–88. doi:10.1007/s00394-008-2009-8PMID 18458837.
  7. Li et al. (May 2010). "Sulforaphane, a dietary component of broccoli/broccoli sprouts, inhibits breast cancer stem cells"Clinical Cancer Research 16 (9): 2580–2590. doi:10.1158/1078-0432.CCR-09-2937PMC 2862133PMID 20388854.

read about synthesis

A Facile and Green Synthesis of Sulforaphane
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by D Tong Jian - 2006 - Cited by 3 - Related articles
A Facile and Green Synthesis of Sulforaphane. Tong Jian DING, Ling ZHOU, Xiao Ping CAO*. Sate Key Laboratory of Applied Organic Chemistry and College of ...






Bingel reaction


Bingel fullerene

The Bingel reaction in fullerene chemistry is a fullerene cyclopropanation reaction to a methanofullerenefirst discovered by C. Bingel in 1993 with the bromo derivative of diethyl malonate in the presence of a basesuch as sodium hydride or DBU.[1] The preferred double bonds for this reaction on the fullerene surface are the shorter bonds at the junctions of two hexagons (6-6 bonds) and the driving force is relief of steric strain.

The reaction is of importance in the field of chemistry because it allows the introduction of useful extensions to the fullerene sphere. These extensions alter their properties for instance solubility and electrochemical behavior and therefore widen the range of potential technical applications.

Reaction mechanism

The reaction mechanism for this reaction is as follows: a base abstracts the acidic malonate proton generating a carbanion or enolatewhich reacts with the electron deficient fullerene double bond in a nucleophilic addition. This in turn generates a carbanion which displaces bromine in a nucleophilic aliphatic substitution in an intramolecular ring cyclopropane ring closure.


The Bingel reaction is a popular method in fullerene chemistry. The malonate (functionalized with the halide atom) is often obtained in situ in a mixture of base and tetrachloromethane or iodine.[2] The reaction is also known to take place with the ester groups replaced byalkyne groups in dialkynylmethanofullerenes.[2]

Bingel reaction of fullerene with a malonate ester and a) sodium hydride or DBUin toluene at room temperature 45% yield.

An alternative to the Bingel reaction is a fullerene diazomethane reaction. N-(Diphenylmethylene)glycinate Esters [3] in a Bingel reaction take a different conjugate course and react to a fullerene dihydropyrrole.

Bingel reaction with N-(Diphenylmethylene)glycinate Ester

Retro-Bingel reaction

Protocols exist for the removal of the methano group based, on electrolytic reduction [4][5] or amalgamated magnesium [6]


  1. Bingel, Carsten (1993). "Cyclopropanierung von Fullerenen". Chemische Berichte 126 (8): 1957. doi:10.1002/cber.19931260829.
  2. Yosuke Nakamura, Masato Suzuki, Yumi Imai, and Jun Nishimura (2004). "16". Org. Lett. 6 (16): 2797–2799.doi:10.1021/ol048952nPMID 15281772.
  3. Graham E. Ball, Glenn A. Burley, Leila Chaker, Bill C. Hawkins, James R. Williams, Paul A. Keller, and Stephen G. Pyne (2005). "Structural Reassignment of the Mono- and Bis-Addition Products from the Addition Reactions of N-(Diphenylmethylene)glycinate Esters to [60]Fullerene under Bingel Conditions". J. Org. Chem. 70 (21): 8572–8574. doi:10.1021/jo051282uPMID 16209611.
  4. Kessinger, Roland; Crassous, Jeanne; Herrmann, Andreas; Rüttimann, Markus; Echegoyen, Luis; Diederich, François (1998). "Preparation of Enantiomerically Pure C76 with a General Electrochemical Method for the Removal of Di(alkoxycarbonyl)methano Bridges from Methanofullerenes: The Retro-Bingel Reaction". Angewandte Chemie International Edition 37 (13-14): 1919.doi:10.1002/(SICI)1521-3773(19980803)37:13/14<1919::AID-ANIE1919>3.0.CO;2-X.
  5. Herranz, M. ÁNgeles; Cox, Charles T.; Echegoyen, Luis (2003). "Retrocyclopropanation Reactions of Fullerenes:  Complete Product Analyses". The Journal of Organic Chemistry 68 (12): 5009. doi:10.1021/jo034102uPMID 12790625.
  6. Moonen, Nicolle N. P.; Thilgen, Carlo; Diederich, François; Echegoyen, Luis (2000). "The chemical retro-Bingel reaction: selective removal of bis(alkoxycarbonyl)methano addends from C60 and C70 with amalgamated magnesium". Chemical Communications (5): 335. doi:10.1039/a909704j.







Substituted indole derivatives for the treatment of immunological disorders, Protein kinase C theta inhibitor WO 2012156936, Novartis AG

Physical properties

Substituted indole derivatives for the treatment of immunological disorders,WO 2012156936, Novartis AG, Protein kinase C theta inhibitor

TITLE-Substituted indole derivatives for the treatment of immunological disorders

Protein kinase C theta inhibitor

WO 2012156936, 22.11.2012, Novartis AG



Phosphoric acid mono-[3-[3-(4,7-diaza-spiro[2.5]oct-7-yl)-isoquinolin-1 -yl]-4-(7-methyl-1 H-indol-3-yl)-2,5-dioxo-2,5-dihydro-pyrrol-1 -ylmethyl] ester

1H-NMR (400 MHz, DMSO-d6): 12.10 (s, 1 H), 8.08 (d, 1 H), 7.65-7.61 (m, 2H), 7.44 (f, 1 H), 7.20 (s, 1 H), 7.06 (f, 1 H), 6.74 (d, 1 H), 6.43 (f, 1 H), 6.00 (d, 1 H), 5.29 (d, 2H), 3.87-3.01 (m, 6H), 2.37 (s, 3H), 0.97-0.62 (m, 4H).

31P-NMR (162 MHz, DMSO-d6): -6.0.

LCMS: [M+1]+ = 574.0, Rt (1) = 1.77 min., Rt (2) = 0.71 min.

Descibed is a  crystalline form of phosphoric acid mono-[3-[3-(4,7-diaza-spiro[2.5]oct-7-yl)-isoquinolin-1- yl]-4-(7-methyl-1 H-indol-3-yl)-2,5-dioxo-2,5-dihydro-pyrrol-1-ylmethyl] ester, especially the mono-hydrate, which preferably has an X-ray powder diffraction pattern with at least one, preferably two, more preferably three, even more preferably four, especially five, most preferably all of the following peaks at an angle of refraction 2 theta (Θ) of 9.525, 16.356, 17.091 , 18.005, 20.859, each ± 0.2

Physical properties

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Jasmone is a natural organic compound extracted from the volatile portion of the oil fromjasmine flowers. It is a colorless to pale yellow liquid that has the odor of jasmine. Jasmone can exist in two isomeric forms with differing geometry around the pentenyl double bond, cis-jasmone and trans-jasmone. The natural extract contains only the cis form, while synthetic material is often a mixture containing both forms, with the cis form predominating. Both forms have similar odors and chemical properties.

Jasmone is produced within plants by the metabolism of jasmonate, from linolenic acid by the octadecanoid pathway. It can act as either an attractant or a repellent for various insects. Commercially jasmone is used primarily in perfumes and cosmetics.

An attempt to make Z jasmone – an important constituent of many perfumes

In fact one synthesis uses the following as carbon sources:

cis (Z) jasmone ,

cas no 488-10-8, 3-methyl-2-[(2Z)-pent-2-en-1-yl]cyclopent-2-en-1-one

ref-(Can. J. Chem. 1978, Vol 56, p2301)

1    W. Theilheimer. Synthetic Methods of Organic Chemistry. Volume 31, 1977, p. 352
2   Tetrahedron, 39 (24), p. 4127, 1983



Predict NMR spectrum


Formula: C10H14O
CAS#: 488-10-8
MW: 150.22









Otamixaban (INN) is a direct factor Xa inhibitor,[1] currently being developed by the French pharmaceutical company Sanofi-Aventis as a treatment for acute coronary syndrome.

Methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate


Guertin KR, Choi YM (2007). “The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development” 

Curr. Med. Chem. 14 (23): 2471–81.doi:10.2174/092986707782023659PMID 17979700.

Methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, (CAS number 193153-04-7) has the International Nonproprietary Name Otamixaban

The present invention (WO2012130821) 4TH OCT 2012, BENZOIC ACID SALT OF OTAMIXABAN, SANOFI relates to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate, and to a benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate which is in a crystalline form or in at least partially crystalline form, as well as a process for the preparation of the same, methods of using such salt to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa and shows the structure illustrated in Formula I:



The benzoic acid salt of methyl (2R,3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1 -oxidopyridin-4-yl)benzoyl]amino}butanoate according to claims 1 to 5 for use in the treatment of acute myocardial infarction, non-ST elevation myocardial infarction, unstable angina, thromboembolism, acute vessel closure associated with thrombolytic therapy, percutaneous transluminal coronary angioplasty, transient ischemic attacks, stroke, intermittent claudication, and restenosis.







Microwave-assisted green synthesis of 1, 3-benzodioxole derivatives

2-Phenyl-substituted 1,3-benzodioxole derivatives were synthesized by microwave irradiation by reacting catechol with benzoic acid derivatives in the presence of polyphosphoric acid as a catalyst which acts as a solvent and also as a cyclizing agent. This synthesis has various advantages over other

Green Chemistry Letters and Reviews

Volume 5Issue 4, 2012


Sayan Dutta Guptet al

pages 609-620

catalytic conventional synthesis because it saves time, increases yield, and is a simple, economical, and effective synthesis. Moreover, this is also an excellent green chemistry approach as it does not require additional toxic solvents or harmful chemicals, and overall it reduced energy utilization than the other methods of synthesis.











anicheck.gif (1995 bytes)






Synthesis of pyrrole derivative from amino gp

synthesis of pyrrole derivative from amino gp,


Paal-Knorr reaction of aniline and 2,5-diketone1-Phenyl-2,5-Dimethylpyrrole

 Reaction Scheme: Paal-Knorr reaction of aniline and 2,5-diketone


To a 250 mL one-necked round bottom flask equipped with stir bar was added aniline (2.79 g, 0.030 mol), 2,5-Hexanedione (3.65 g, 0.032 mol), and toluene (75 mL, 0.4 M in aniline). Upon mixing for 5 minutes, p-TsOH (0.114 g, 0.0006 mol) was added all at once. The flask was then equipped with a Dean-Stark trap and reflux condenser. The solution was heated to reflux (≈120oC). for 1 houra. After this time the flask was cooled to room temperature and the solution was  transferred to a 500 mL separatory funnel. The organic layer was washed with a saturated sodium bicarbonate solution (2 X 100 mL), deionized water (2 X 100 mL), and finally with brine (2 X 100 mL).  The organic layer was dried with Na2SOand the solvent was removed by rotary evaporation to afford a greenish solidb,c (3.69 g, 72%). 

a.  By this time approximately  one equivalent (based on aniline) of water had condensed into the Dean-Stark trap. 
b. This was judged to be pure by GC-MS and NMR analysis
c. Despite these colorations, their GC-MS and NMR data agreed with literature data


1H NMR (CDCl3, 300 MHz) δ ppm 2.03 (s, 3 H) 5.91 (s, 2 H) 7.19-7.22-(m, 2 H) 7.38-7.47 (m,3 H) 7.37 (d, J=8.80 Hz, 2 H) 
13C NMR (CDCl3, 75 MHz) δ ppm 13.12 (CH3) 105.82 (CH) 127.72 (C) 128.36 (CH) 128.83 (CH) 129.15 (CH)  139.15 (C)

Thiemann, F.; Piehler, T.; Haase, D.; Saak, W.; Lützen A. Eur. J. Org. Chem. 2005, 1991.







Gram amounts of “nanohoops”

Preparation of carbon nanotubes as pure substances could benefit from a new way to make gram amounts of “nanohoops” (Chem. Sci., DOI:10.1039/c2sc20719b).


Nanohoops—or cycloparaphenylenes (CPPs)—are like bracelets made from para-linked benzene rings. Stacking of CPPs could be the basis for preparing useful quantities of pure carbon nanotubes.

Sizable quantities of [8]CPP and [10]CPP are now accessible, potentially easing the way to carbon nanotube synthesis. The armchair carbon nanotube image shows how two [8]CPPs (red and black bold) could be linked to begin forming the nanotube.
This figure shows structures of [8]CPP and [10]CPP. The [8]CPP rings can link to make an armchair carbon nanotube, also shown.

Synthetic organic chemist Ramesh Jasti—then in Carolyn R. Bertozzi’s group at Lawrence Berkeley National Laboratory’s Molecular Foundry—and coworkers first synthesized CPPs catalytically in 2008

  J. Am. Chem. Soc., DOI: 10.1021/ja807126u).


But the catalysts they used weren’t ideal, and yields of CPPs were low. CPPs have remained so difficult to make that they are currently sold commercially for about $100 per milligram.






The Fráter-Seebach alkylation

The Fráter-Seebach alkylation is the stereoselective alkylation of chiral beta-hydroxy esters using superbases such as LDA or LiHMDS. This organic reaction was first reported by G. Fráter in 1979 (DOI DOI). 

In the original Fráter publication the starting material is ethyl acetoacetate 1, stereoselectively converted to the beta-hydroxy ester 2 with Baker's yeast, converted to the dianion 3 with LDA and finally alkylated with iodomethanein HMPA to 4. 





Novel Method for Enantioseparation of Drugs (Clenbuterol)

thumbnail image: Novel Method for Enantioseparation of Drugs


Carbon nanotubes (CNTs) have attracted considerable interest due to their unique structure and remarkable properties. Racemic drugs normally contain only one enantiomer that is active, and to get enantiomerically pure drugs to the market is always an urgent task. As promising reagents, chiral selector modified CNTs have been successfully used to separate enantiomers.

Jingang Yu and colleagues, Central South University, China, proposed a novel method to functionalize multi-walled carbon nanotubes (MWCNTs) with hydroxypropyl-β-cyclodextrin (HP-β-CD). These modified multi-walled nanotube samples were fully characterized.

MWCNT-HP-β-CD was used as thin-layer chromatography stationary phase additive to separate clenbuterol enantiomers with satisfactory results. The presence of CNTs permits a higher recognition of enantiomers, so chiral selector modified CNTs have a promising application in resolution of chiral molecules.

Preparation of Hydroxypropyl-β-cyclodextrin Cross-linked Multi-walled Carbon Nanotubes and Their Application in Enantioseparation of Clenbuterol
J. Yu, D. Huang, K. Huang, Y. Hong,
Chinese J. Chem. 201129(5), 893—897.
DOI: 10.1002/cjoc.201190185







Chiral Separation of Ibuprofen to (S)-ibuprofen

Chiral Separation by a Pseudo Membrane in a Triple-Laminar Flow with a Microfluidic Contactor
T.-H. Yoon, L.-Y. Hong, D.-P. Kim,
Chem. Asian J. 2011.
DOI: 10.1002/asia.201000798

thumbnail image: Chiral Separation of Ibuprofen


The pharmacological activity of ibuprofen, a common painkiller and anti-inflammatory drug, arises predominantly from its (S)-form. Separation of the (R)- and (S)-forms is difficult as they differ only in optical polarity.

The continuous and simultaneous reaction/separation of ibuprofen racemate has been reported by Dong-Pyo Kim and co-workers, Chungnam National University, South Korea. They use an inorganic polymer-chip device with triple-laminar flow. A feed phase withCandida rugosa lipase was used to facilitate esterification of (S)-ibuprofen due to its selective chiral recoginition and resolution. The (S)-ibuprofen ester was then transported through an ionic liquid which acted as a pseudo-membrane. Finally, conversion into (S)-ibuprofen was achieved by H2SO4 acid hydrolysis in a receiving stream.

The separated ibuprofen revealed very high chiral purity, with 99.9 % enantiomeric excess throughout the process conditions








One-step conversion of unprotected sugars to β-glycosyl azides using 2-chloroimidazolinium salt in aqueous solution

One-step conversion of unprotected sugars to -glycosyl azides using 2-chloroimidazolinium salt in aqueous solution
Tomonari Tanaka, Hikaru Nagai, Masato Noguchi, Atsushi Kobayashi and Shin-ichiro Shoda,  Chem. Commun., 2009, 3378
DOI: 10.1039/b905761g


graphical abstract image (ID: b905761g)

Various -glycosyl azides have been synthesized directly in water by the reaction of unprotected sugars and sodium azide mediated by 2-chloro-1,3-dimethylimidazolinium chloride.







The Top 10 Aphrodisiac Foods

The Top 10 Aphrodisiac Foods

Asparagus, honey, bananas and other foods can get you in the mood and help get your blood flowing down to your sexy parts.

You are what you eat, because what you eat directly influences your body and your body functions.

The food you consume can have a direct impact on your sex life, affecting your hormones, brain chemistry and energy and stress levels. Some foods have psychoactive properties, others arouse because they are psychologically suggestive, and some can actually increase blood flow to the genitals. And if it does not have all that aphrodisiac effect, at least it’s healthy and it will do you good!




top-10-aphrodisiac-foods01 Top 10 Aphrodisiac Foods

An English herbalist from the 17th century, Nicholas Culpepper, wrote that asparagus "stirs up lust in man and woman." In 19th century France, bridegrooms were served three courses of the sexy spears at their prenuptial dinners. Apparently for a good reason: asparagus is a great source of potassium, fiber, vitamin B6, vitamins A and C, and thiamin and folic acid. The latter is said to boost histamine production necessary for the ability to reach orgasm in both sexes.



top-10-aphrodisiac-foods02 Top 10 Aphrodisiac Foods

Through antiquity, almonds were regarded as fertility symbols. The aroma of almond supposedly arouses passion in females -- or so thought the poets and scribes. The scientists say that almonds provide high doses of vitamin E, magnesium and even fiber. Therefore, there seems to be something in the almond myths after all.



top-10-aphrodisiac-foods03 Top 10 Aphrodisiac Foods

Just by looking at the shape of avocado, you will see the reason why it was associated with sexuality. The Aztecs called the avocado ahuacuatl, or "testicle tree." They thought the fruit hanging in pairs on the tree resembled testicles. The Catholic priests in Spain found this fruit so obscenely sexual that they forbade it. On the other side, avocado is rich with folic acid, vitamin B6 and potassium. They are also said to boost immune system.



top-10-aphrodisiac-foods04 Top 10 Aphrodisiac Foods

By it shape its connection with sexuality is quite obvious, but you’ll also find that bananas are loaded with potassium, magnesium and B vitamins. It also contains chelating minerals and the bromeliad enzyme, said to enhance the male libido.


6 -- BASIL

top-10-aphrodisiac-foods05 Top 10 Aphrodisiac Foods

Basil not only makes the meals smell and taste better, but it also has a lot of beneficial effects on human body. Basil has a fantastic aroma that is said to have an aphrodisiac effect; it is also very stimulating. Using sweet basil in a pasta sauce will be sure to get your heart racing! Maybe this explains why Italians are so romantic!



top-10-aphrodisiac-foods06 Top 10 Aphrodisiac Foods

Pure chocolate, the king of natural aphrodisiacs, contains a host of compounds including anandamide, the psyochoactive feel-good chemical, and PEA (phenylethylamine), the "love chemical," which releases dopamine in the pleasure centers of the brain and peaks during orgasm. PEA is said to help induce feelings of excitement, attraction and euphoria. Cacao also contains tryptophan, a key component of the neurotransmitter serotonin known to promote a sense of well-being and relaxation.


4 -- FIGS

top-10-aphrodisiac-foods07 Top 10 Aphrodisiac Foods

This sexy fruit has long been thought of as an arousing stimulant, and an open fig is believed to emulate the female sex organs. Figs are steeped in history and are one of the oldest-recorded fruits. They are mentioned in the Bible (Adam and Eve wore fig leaves to cover their private parts), are reported to be Cleopatra’s favorite fruit, and the ancient Greeks held them as sacred and associated them with love and fertility.



top-10-aphrodisiac-foods08 Top 10 Aphrodisiac Foods

Now, wait a minute! I know it’s stinky, but more importantly it’s strong, which is exactly what it will happen to guys. Garlic is chockfull of allicin, an ingredient that will increase blood flow. So, whip up an extra-garlicky dish and keep the Altoids handy.



top-10-aphrodisiac-foods09 Top 10 Aphrodisiac Foods

Oysters are probably the food most associated with being an aphrodisiac, and most people are aware of their reputation for increasing sexual desire. Oysters may be thought an aphrodisiac because of their high zinc content, which helps produce sperm and increases libido. Raw oysters are best served with a glass of chilled Champagne for a truly romantic meal!



1 -- HONEY

top-10-aphrodisiac-foods10 Top 10 Aphrodisiac Foods

Sweet, sticky honey is a great source of boron, a trace mineral that helps the body use and metabolize estrogen, the female sex hormone. Studies have shown that this mineral may also enhance testosterone levels in the blood, the hormone responsible for promoting sex drive and orgasm in both men and women. In addition, honey contains B vitamins needed for testosterone, as well as other nutrients, enzymes and phytochemicals.








Carbohydrate chemistry in drug discovery

Carbohydrate chemistry in drug discovery

M. Carmen Galan ,  David Benito-Alifonso and Gregory M. Watt


Affiliation Information 


1. School of Chemistry,University of Bristol,Cantock's Close, Bristol, U.K


Org. Biomol. Chem., 2011, 9, 3598-3610


The multitude of roles that carbohydrates and their glyco-conjugates play in biological processes has stimulated great interest in determining the nature of their interactions in both normal and diseased states.

Graphical abstract: Carbohydrate chemistry in drug discovery










Brevetoxin (PbTx), or brevetoxins, are a suite of cyclic polyether compoundsproduced naturally by a species of dinoflagellate known asKarenia brevis.Brevetoxins are neurotoxins that bind to voltage-gated sodium channels in nervecells, leading to disruption of normal neurological processes and causing theillness clinically described as neurotoxic shellfish poisoning (NSP).Although brevetoxins are most well-studied in K. brevis, they are also found inother species of Karenia and at least one large fish kill has been traced tobrevetoxins in Chattonella







New developments on the cheminformatics open workflow environment CDK-Taverna

New developments on the cheminformatics open workflow environment CDK-Taverna


Andreas Truszkowski, Kalai Vanii Jayaseelan, Stefan Neumann, Egon L Willighagen, Achim Zielesny, Christoph SteinbeckJournal of Cheminformatics 2011, 3:54 (13 December 2011)

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