The Challenge of Atropisomerism in Drug Discovery

被引：625

作者：

Clayden, Jonathan ^{[1
]}

Moran, Wesley J. ^{[1
]}

Edwards, Paul J. ^{[2
]}

LaPlante, Steven R. ^{[2
]}

机构：

[1] Univ Manchester, Sch Chem, Manchester M13 9PL, Lancs, England

[2] Boehringer Ingelheim Canada Ltd, Dept Chem, Laval, PQ H7S 2G5, Canada

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2009年 / 48卷 / 35期

基金：

英国工程与自然科学研究理事会;

关键词：

atropisomerism; chirality; conformers; drug discovery; kinetics; BIOLOGICAL EVALUATION; CHIRAL INVERSION; BOND ROTATION; ANTAGONISTS; INTERCONVERSION; OPTIMIZATION; ENANTIOMERS; HYDROLYSIS; MODULATION; BLOCKERS;

D O I：

10.1002/anie.200901719

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A twist in the tale: Recent reports have highlighted solutions to the problems encountered when drug candidates exist as slowly interconverting conformers or atropisomers (see scheme). This Minireview brings together the various strategies that have been adopted and proposes a general approach to handling an aspect of stereochemistry which has received little attention from drug regulatory agencies. © 2009 Wiley-VCH Verlag GmbH & Co. KCaA.

引用

页码：6398 / 6401

页数：4

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