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β-GLUCAN . Food Ingredient Sourced From Yeast, Shanghai Genon Biotech Co.,Ltd « New Drug Approvals

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PATENT EXPIRY DATES « New Drug Approvals

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PATENT EXPIRY DATES « New Drug Approvals

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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.

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