NEW DRUG APPROVALS ACHIEVES ONE LAKH VIEWS IN 166 COUNTRIES « New Drug Approvals

NEW DRUG APPROVALS ACHIEVES ONE LAKH VIEWS IN 166 COUNTRIES « New Drug Approvals:

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Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

Med. Chem. Commun., 2013, 4,1323-1343
DOI: 10.1039/C3MD00152K, Review Article

Davide Garella, Emily Borretto, Antonella Di Stilo, Katia Martina, Giancarlo Cravotto, Pedro Cintas
Microwave-assisted synthesis of heterocycle libraries has given an impressive contribution to drug discovery and development.http://pubs.rsc.org/en/Content/ArticleLanding/2013/MD/C3MD00152K?utm_source=feedburner&utm_medium=feed&utm_campaign=Feed%3A+rss%2FMD+%28RSC+-+Med.+Chem.+Commun.+latest+articles%29#!divAbstract

 

Microwave-assisted synthesis of N-heterocycles in medicinal chemistry

 

 

 The syntheses of almost all N-heterocycles have now been successfully performed under microwave irradiation and have provided significant improvements in the reaction time and efficiency. The peculiar properties of dielectric heating give it the ability to strongly promote cyclocondensation, cycloaddition and selective N-heterocycle functionalisation and it has, therefore, very much caught the attention of the medicinal chemistry community. In this work, we present an overview of recent literature and technical advances in this research field with the aim of providing insight into the applications of microwave-assisted synthesis in the preparation of the main drug categories that contain N-heterocycle scaffolds.

A Novel Solid-Phase Synthesis of Quinolines

Short Paper | Regular issue | Vol 85, No. 3, 2012, pp.667-676
Published online: 26th January, 2012

DOI: 10.3987/COM-11-12411

■ A Novel Solid-Phase Synthesis of Quinolines

E Tang,* Deshou Mao, Wen Li, Zhangyong Gao, and Pengfei Yao

*School of Chemical Science and Technology, Yunnan University, No. 2 Green Lake North Road, Kunming 650091, China

Abstract

A method for synthesizing substituted-quinolines using TMSOTf-catalyzed polystyrene-supported succinimidyl selenide-induced intramolecular seleno-arylation of tethered alkenes as a key step has been developed. The catalytic process provides an efficient method for the stereoselective and regioselective synthesis of tetrahydroquinoline possessing a seleno-functionality, followed by deprotection of tosyl group and syn-elimination of selenoxides to provide quinolines in good yields and purities.

 http://www.heterocycles.jp/newlibrary/payments/form/22246/fulltext

Efficient Synthesis of 2,4-Diarylquinolines via Fe(III) Trifluoroacetate Catalyzed Three-Component Reactions under Solvent-Free Conditions

 

 

Paper | Regular issue | Vol 85, No. 3, 2012, pp.639-649
Published online: 9th February, 2012

DOI: 10.3987/COM-12-12433

■ Efficient Synthesis of 2,4-Diarylquinolines via Fe(III) Trifluoroacetate Catalyzed Three-Component Reactions under Solvent-Free Conditions

Min Zhang,* Ting Wang, Biao Xiong, Fengxia Yan, Xiaoting Wang, Yuqiang Ding, and Qijun Song

*School of Chemistry and Materials Engineering, Jiangnan University, 1800 Lihu Road, Wuxi, Jiangsu Province, 214122, China

Abstract

A convenient and efficient one-pot synthesis of 2,4-diarylquinolines is described by using Fe(CF3CO2)3 as a catalyst for the first time. In this method, three-component coupling of arylaldehydes, arylamines and arylacetylenes furnished the corresponding products in good to excellent yields. The work features the use of cheap and eco-friendly catalyst, excellent functional group tolerance and solvent-free conditions. A variety of new products were afforded effectively.

http://www.heterocycles.jp/newlibrary/payments/form/22272/fulltext

ALKALOIDS

Alkaloids from Indian Foundation For Rediscovering traditional knowledge

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Photosynthesis: Turning CO2 into O2 – or maybe not. | DownHouseSoftware

Photosynthesis: Turning CO2 into O2 – or maybe not. | DownHouseSoftware:

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GSK and Genmab seek alternative approval for leukaemia drug Arzerra « New Drug Approvals

GSK and Genmab seek alternative approval for leukaemia drug Arzerra « New Drug Approvals:

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