The challenge of atropisomerism in drug discovery

Jonathan Clayden; Wesley J. Moran; Paul J. Edwards; Steven R. Laplante

doi:10.1002/anie.200901719

The challenge of atropisomerism in drug discovery

Jonathan Clayden^*, Wesley J. Moran, Paul J. Edwards, Steven R. Laplante

^*Corresponding author for this work

School of Chemistry

Research output: Contribution to journal › Article (Academic Journal) › peer-review

588 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	6398-6401
Number of pages	4
Journal	Angewandte Chemie - International Edition
Volume	48
Issue number	35
Early online date	27 Jul 2009
DOIs	https://doi.org/10.1002/anie.200901719
Publication status	Published - 17 Aug 2009

Keywords

Atropisomerism
Chirality
Conformers
Drug discovery
Kinetics

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KW - Kinetics

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The challenge of atropisomerism in drug discovery

Abstract

Keywords

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