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探索“实用”的边界:基于复杂天然产物的新药候选物的从头合成。

Exploring the Boundaries of "Practical": De Novo Syntheses of Complex Natural Product-Based Drug Candidates.

机构信息

Department of Chemistry and Biochemistry, University of California-Los Angeles , 607 Charles E. Young Drive East, Los Angeles, California 90095-1569, United States.

出版信息

Chem Rev. 2017 Sep 27;117(18):11994-12051. doi: 10.1021/acs.chemrev.7b00126. Epub 2017 Jun 12.

Abstract

This review examines the state of the art in synthesis as it relates to the building of complex architectures on scales sufficient to drive human drug trials. We focus on the relatively few instances in which a natural-product-based development candidate has been manufactured de novo, rather than semisynthetically. This summary provides a view of the strengths and weaknesses of current technologies, provides perspective on what one might consider a practical contribution, and hints at directions the field might take in the future.

摘要

本文综述了与构建足够规模的复杂结构以推动人体药物试验相关的合成技术的最新进展。我们重点关注了极少数情况下基于天然产物的开发候选物是全新合成的,而不是半合成的情况。本文总结了当前技术的优缺点,提供了对实际贡献的看法,并暗示了该领域未来可能的发展方向。

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