Chemical Development, GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK.
Department of Pure and Applied Chemistry WestCHEM, University of Strathclyde, 295 Cathedral Street, Glasgow, Scotland, G1 1XL, UK.
Chemistry. 2021 Jan 4;27(1):158-174. doi: 10.1002/chem.202002849. Epub 2020 Oct 8.
Exploration of novel, three-dimensional chemical space is of growing interest in the drug discovery community and with this comes the challenge for synthetic chemists to devise new stereoselective methods to introduce chirality in a rapid and efficient manner. This Minireview provides a timely summary of the development of palladium-catalyzed asymmetric redox-relay Heck-type processes. These reactions represent an important class of transformation for the selective introduction of remote stereocenters, and have risen to prominence over the past decade. Within this Minireview, the vast scope of these transformations will be showcased, alongside applications to pharmaceutically relevant chiral building blocks and drug substances. To complement this overview, a mechanistic summary and discussion of the current limitations of the transformation are presented, followed by an outlook on future areas of investigation.
探索新颖的三维化学空间在药物发现领域越来越受到关注，随之而来的挑战是合成化学家需要设计新的立体选择性方法，以便快速有效地引入手性。这篇综述及时总结了钯催化不对称氧化还原接力 Heck 型反应的发展。这些反应代表了一类用于选择性引入远程立体中心的重要转化，在过去十年中受到了广泛关注。在这篇综述中，将展示这些转化的广泛应用范围，以及在手性药物相关构建块和药物物质中的应用。为了补充这一概述，还介绍了该转化的机制总结和当前限制的讨论，并对未来的研究领域进行了展望。
