DR ANTHONY MELVIN CRASTO,WorldDrugTracker, helping millions, A 90 % paralysed man in action for you, I am suffering from transverse mylitis and bound to a wheel chair, With death on the horizon, nothing will not stop me except God
DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 25Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK GENERICS at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution
n

Saturday, 7 May 2016

N-Butylpyrrolidinone as a dipolar aprotic solvent for organic synthesis


Green Chem., 2016, Advance Article
DOI: 10.1039/C6GC00932H, Paper
James Sherwood, Helen L. Parker, Kristof Moonen, Thomas J. Farmer, Andrew J. Hunt
N-Butylpyrrolidinone (NBP) has been demonstrated as a suitable safer replacement solvent for N-Methylpyrrolidinone (NMP) in selected organic syntheses.

N-Butylpyrrolidinone as a dipolar aprotic solvent for organic synthesis

*Corresponding authors
aGreen Chemistry Centre of Excellence, Department of Chemistry, University of York, UK
E-mail: andrew.hunt@york.ac.uk
bEastman Chemical Company, Pantserschipstraat 207 – B-9000, Gent, Belgium
Green Chem., 2016, Advance Article
DOI: 10.1039/C6GC00932H
 
Dipolar aprotic solvents such as N-methylpyrrolidinone (or 1-methyl-2-pyrrolidone (NMP)) are under increasing pressure from environmental regulation. NMP is a known reproductive toxin and has been placed on the EU “Substances of Very High Concern” list. Accordingly there is an urgent need for non-toxic alternatives to the dipolar aprotic solvents. N-Butylpyrrolidinone, although structurally similar to NMP, is not mutagenic or reprotoxic, yet retains many of the characteristics of a dipolar aprotic solvent. This work introduces N-butylpyrrolidinone as a new solvent for cross-coupling reactions and other syntheses typically requiring a conventional dipolar aprotic solvent.

str1
////N-Butylpyrrolidinone, dipolar aprotic solvent , organic synthesis

Saturday, 30 April 2016

Dehydrogenative [2 + 2 + 1] Heteroannulation Using a Methyl Group as a One-Carbon Unit: Access to Pyrazolo[3,4-c]quinolines

 Figure

State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, China
State Key Laboratory of Applied Organic Chemistry Lanzhou University, Lanzhou 730000, China
Org. Lett., Article ASAP
DOI: 10.1021/acs.orglett.6b00618
Publication Date (Web): April 28, 2016
Copyright © 2016 American Chemical Society
*E-mail: srj0731@hnu.edu.cn., *E-mail: jhli@hnu.edu.cn.
 A practical and straightforward access to pyrazolo[3,4-c]quinolines by molecular sieve mediated dehydrogenative [2 + 2 + 1] heteroannulation of N-(o-alkenylaryl)imines with aryldiazonium salts is described using a sp3-hybrid carbon atom as a one-carbon unit. The reaction enables the formation of three new chemical bonds, a C–C bond and two C–N bonds, in a single reaction and features simple operation and excellent functional group tolerance.





/////////Dehydrogenative [2 + 2 + 1] Heteroannulation,   Pyrazolo[3,4-c]quinolines

Wednesday, 6 April 2016

Continuous-Flow Process for the Synthesis of m-Nitrothioanisole


Abstract Image
A continuous-flow process for the preparation of m-nitrothioanisole has been set up. The starting material m-nitroaniline was diazotized to give diazonium chloride, followed by azo-coupling with sodium thiomethoxide to give 1-(methylthio)-2-(3-nitrophenyl)diazene, then dediazoniated to gain m-nitrothioanisole in high yield. The continuous-flow process minimized accumulation of the energetic intermediate diazonium salt and has a better capacity for adapting large-scale production. A solvent was introduced in the azo-coupling section to create a biphasic flow system. Side products were inhibited eminently in this flow process.



Continuous-Flow Process for the Synthesis of m-Nitrothioanisole

Zhiqun Yu, Xiaoxuan Xie, Hei Dong, Jiming Liu, and Weike Su*
National Engineering Research Center for Process Development of Active Pharmaceutical Ingredients, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, P. R. China
Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, P. R. China
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/acs.oprd.6b00023
Publication Date (Web): March 24, 2016
Copyright © 2016 American Chemical Society
*Tel.: (+86)57188320899. E-mail: pharmlab@zjut.edu.cn.
http://pubs.acs.org/doi/abs/10.1021/acs.oprd.6b00023
////////

Monday, 21 March 2016

Eco-friendly construction of highly functionalized chromenopyridinones by an organocatalyzed solid-state melt reaction and their optical properties


Green Chem., 2016, 18,1488-1494
DOI: 10.1039/C5GC02658J, Paper
Sanjay Paul, Yong Rok Lee
Diverse chromenopyridinone derivatives were synthesized under organocatalytic solid-state melt conditions. The optical properties of these [small pi]-expanded chromenopyridine derivatives were examined.
The content of this RSS Feed (c) The Royal Society of Chemistry


http://pubs.rsc.org/en/Content/ArticleLanding/2016/GC/C5GC02658J?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FGC+%28RSC+-+Green+Chem.+latest+articles%29#!divAbstract

Eco-friendly construction of highly functionalized chromenopyridinones by an organocatalyzed solid-state melt reaction and their optical properties

Sanjay Paula and   Yong Rok Lee*a  
*
Corresponding authors
a
School of Chemical Engineering, Yeungnam University, Gyeongsan 712-749, Republic of Korea
E-mail: yrlee@yu.ac.kr
Fax: +82-53-810-4631
Tel: +82-53-810-2529
Green Chem., 2016,18, 1488-1494

DOI: 10.1039/C5GC02658J


















The library construction of highly functionalized and diverse chromenopyridinones was achieved by three-component reactions of various 4-hydroxycoumarins with ammonium acetate and 3-formylchromones under L-proline catalyzed solid-state melt conditions. The advantages of this protocol include the use of an inexpensive organocatalyst, avoidance of toxic organic solvents, environmentally benign conditions, an easy work-up procedure and good to excellent product yields. The optical properties of these π-expanded varieties of the synthesized chromenopyridinone derivatives were also examined. A chromeno[4,3-b]pyridine nucleus bearing an electron donating group exhibited strong emission in the blue-green region of the visible spectrum.









////////

Saturday, 12 March 2016

High Trans Kinetic Selectivity in Ruthenium-Based Olefin Cross-Metathesis through Stereoretention

Abstract Image.







High Trans Kinetic Selectivity in Ruthenium-Based Olefin Cross-Metathesis through Stereoretention

The Arnold and Mabel Beckman Laboratory of Chemical Synthesis, Division of Chemistry and Chemical Engineering. California Institute of Technology, Pasadena, California 91125, United States
Materia, Inc., Pasadena, California 91107, United States
Org. Lett., 2016, 18 (4), pp 772–775
DOI: 10.1021/acs.orglett.6b00031
Publication Date (Web): February 03, 2016
Copyright © 2016 American Chemical Society

 http://pubs.acs.org/doi/abs/10.1021/acs.orglett.6b00031





//////////

Wednesday, 17 February 2016

The Medicinal Chemistry of Dengue Virus

Abstract Image



The dengue virus and related flaviviruses are an increasing global health threat. In this perspective, we comment on and review medicinal chemistry efforts aimed at the prevention or treatment of dengue infections. We include target-based approaches aimed at viral or host factors and results from phenotypic screenings in cellular assay systems for viral replication. This perspective is limited to the discussion of results that provide explicit chemistry or structure–activity relationship (SAR), or appear to be of particular interest to the medicinal chemist for other reasons. The discovery and development efforts discussed here may at least partially be extrapolated toward other emerging flaviviral infections, such as West Nile virus. Therefore, this perspective, although not aimed at flaviviruses in general, should also be able to provide an overview of the medicinal chemistry of these closely related infectious agents.


READ AT
http://pubs.acs.org/doi/full/10.1021/acs.jmedchem.5b01653


The Medicinal Chemistry of Dengue Virus

Medicinal Chemistry, Institute of Pharmacy and Molecular Biotechnology IPMB, Heidelberg University, Im Neuenheimer Feld 364, 69120 Heidelberg, Germany
§ Laboratory of Organic Synthesis, Institute of Chemistry of the Academy of Sciences of Moldova, Academiei 3, 2028 Chisinau, Moldova
J. Med. Chem., Article ASAP
DOI: 10.1021/acs.jmedchem.5b01653
Publication Date (Web): January 15, 2016
Copyright © 2016 American Chemical Society
*C. D. Klein, phone +49-6221-544875, e-mail c.klein@uni-heidelberg.de.
ACS Editors' Choice - This is an open access article published under an ACS AuthorChoice License, which permits copying and redistribution of the article or any adaptations for non-commercial purposes.

Biography
Mira A. M. Behnam studied pharmacy and biotechnology at The German University in Cairo, where she obtained her B.Sc. degree (2009) and M.Sc. degree (2011) in Pharmaceutical Chemistry in collaboration with Würzburg University. Since 2013, she is DAAD scholarship holder and Ph.D. candidate in the group of Prof. Christian Klein (Heidelberg University) working on the development of potent antiviral compounds against dengue and West Nile virus.
Biography
Christoph Nitsche studied chemistry and business administration. He obtained his Ph.D. on the development of dengue virus protease inhibitors under the guidance of Prof. Christian Klein at Heidelberg University with a scholarship from the German National Academic Foundation. Currently, he is working as a Feodor Lynen Fellow (Alexander von Humboldt-Foundation) in the laboratory of Prof. Gottfried Otting at the Australian National University. His present research focuses on novel NMR methods for drug discovery.
Biography
Veaceslav Boldescu studied pharmaceutical technology and obtained a Ph.D. in Technology of special products (pharmaceuticals) in 2008 under the guidance of Acad. Gheorghe Duca (Academy of Sciences of Moldova). He started his research pathway at the State University of Moldova and continued it at the Institute of Chemistry of the Academy of Sciences of Moldova, working in the Laboratory of Organic Synthesis lead by Prof. Fliur Macaev. His main research interests include development of new chemotherapeutic agents against infections such as tuberculosis and dengue.
Biography
Christian D. Klein studied pharmacy and obtained a Ph.D. in Pharmaceutical Chemistry in 2000 under the guidance of Profs. Ulrike Holzgrabe (University of Bonn) and A. J. Hopfinger (UIC, Chicago). Following postdoctoral work at ETH Zürich, he became an Emmy Noether junior group leader. Since 2007, he is professor of Pharmaceutical Chemistry at Heidelberg University. His main research interests are anti-infective compounds and fundamental questions in medicinal chemistry, such as the study of unusual binding modes and structural motifs.

////

Monday, 11 January 2016

Continuous ruthenium-catalyzed methoxycarbonylation with supercritical carbon dioxide




Catal. Sci. Technol., 2016, Advance Article
DOI: 10.1039/C5CY01883H, Paper
Stefan Christiaan Stouten, Timothy Noel, Qi Wang, Matthias Beller, Volker Hessel
The methoxycarbonylation of cyclohexene with carbon dioxide over a ruthenium catalyst was realized in a micro flow system under supercritical conditions.

Continuous ruthenium-catalyzed methoxycarbonylation with supercritical carbon dioxide

The methoxycarbonylation of cyclohexene with carbon dioxide over a ruthenium catalyst was realized in a micro flow system under supercritical conditions. Instead of the toxic and flammable carbon monoxide, this process utilizes carbon dioxide, thereby avoiding issues with bulk transportation of carbon monoxide as well as eliminating the need for safety precautions associated with the use of carbon monoxide. Obtained was a 77% yield of the ester product at 180 °C, 120 bar and with a 90 min residence time, which is over five times faster than for the same reaction performed under subcritical conditions in batch. An important factor for the performance of the system was to have a sufficiently polar supercritical mixture, allowing the catalyst to dissolve well. The optimal temperature for the reaction was 180 °C, as the activity of the system dropped considerably at higher temperatures, most likely due to catalyst deactivation.


Department of Chemical Engineering and Chemistry

ir. S.C. (Stefan) Stouten –

Stouten, ir. S.C.
Address:
Technische Universiteit Eindhoven
P.O. Box 513
5600 MB EINDHOVEN
Department:
Department of Chemical Engineering and Chemistry
Section:
Micro Flow Chemistry and Process Technology
Positioncategory:
doctoral candidate (PhD) (PhD Stud.)
Position:
doctoral candidate
Room:
STW 0.
Email:
s.stouten@tue.nl



Volker Hessel

prof.dr. V. (Volker) Hessel

Hessel, prof.dr. V.
Address:
Technische Universiteit Eindhoven
P.O. Box 513
5600 MB EINDHOVEN
Chair:
Micro Flow Chemistry and Process Technology
Department:
Department of Chemical Engineering and Chemistry
Section:
Micro Flow Chemistry and Process Technology
Positioncategory:
Professor (HGL)
Position:
Full Professor
Room:
STW 1.45
Tel:
+31 40-247 2973
Tel (internal):
2973
Email:
v.hessel@tue.nl
////////Continuous,  ruthenium-catalyzed,  methoxycarbonylation, supercritical carbon dioxide, flow reactor