大学化学 >> 2023, Vol. 38 >> Issue (10): 313-323.doi: 10.3866/PKU.DXHX202301033

未来化学家 上一篇    下一篇

分子骨架编辑在药物合成中的应用与展望

贺静远1, 王泽铠1, 戚显玮1, 陈开元2, 卞江1,*()   

  1. 1 北京大学化学与分子工程学院, 北京 100871
    2 北京大学物理学院, 北京 100871
  • 收稿日期:2023-01-26 录用日期:2023-05-08 发布日期:2023-05-12
  • 通讯作者: 卞江 E-mail:bj@pku.edu.cn

Application and Prospect of Molecular Skeletal Editing in Drug Synthesis

Jingyuan He1, Zekai Wang1, Xianwei Qi1, Kaiyuan Chen2, Jiang Bian1,*()   

  1. 1 College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China
    2 School of Physics, Peking University, Beijing 100871, China
  • Received:2023-01-26 Accepted:2023-05-08 Published:2023-05-12
  • Contact: Jiang Bian E-mail:bj@pku.edu.cn

摘要:

分子编辑是有机合成领域亘古不变的研究热点,其包括外围编辑与骨架编辑。在过去,分子编辑往往着重于C―H键的外围编辑,而骨架编辑则是近年来新兴起的方法学。这一类反应操作简单,专一性强,可以大幅简化合成路线,在药物合成与开发领域应用广泛。本文基于常见的几类分子编辑反应,通过与传统方法对比的方式介绍两例分子骨架编辑在药物合成中的应用,并通过对该领域前沿发展的介绍,对该方法学的未来应用进行展望。

关键词: 分子编辑, 骨架编辑, 药物合成, 药物开发

Abstract:

Molecular editing, including peripheral and skeletal editing, is an area of interest in the field of organic synthesis. Typically, the peripheral editing of C―H bonds is conventionally used for molecular editing. By contrast, skeletal editing is a novel method, which has broader applications in total synthesis and drug development, with advantages of easy operation, high specificity, and simple synthetical routes. This review introduces two skeletal editing examples using common reactions. By comparisons with conventional methods, the applications of molecular editing in drug synthesis are revealed. Moreover, this review predicts the future applications of molecular editing by presenting some state-of-the-art developments in this field.

Key words: Molecular editing, Skeletal editing, Drug synthesis, Drug development