2-苯基环丙胺类衍生物合成研究进展  

Progress in the Synthesis of 2-Phenylcyclopropylamine Derivatives

作　　者：张静雅 王艺霞 郜文硕 余斌[1,2] ZHANG Jingya;WANG Yixia;GAO Wenshuo;YU Bin(School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001;Key Lab.of Advanced Drug Preparation Technologies,Ministry of Education,Zhengzhou University,Zhengzhou 450001)

机构地区：[1]郑州大学药学院,河南郑州450001 [2]郑州大学,药物关键制备技术教育部重点实验室,河南郑州450001

出　　处：《中国医药工业杂志》2023年第6期813-824,共12页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金项目(81973177);河南省优秀青年科学基金项目(222300420069);河南省高校科技创新人才支持计划(21HASTIT045)。

摘　　要：2-苯基环丙胺及其衍生物是合成抗肿瘤药、抗抑郁药和抗凝血药等的重要手性中间体。其合成途径主要包括由环丙烷类衍生物直接合成和从头构建环丙烷策略(如Corey-Chaykovsky反应、Kulinkovich-de Meijere反应等)。文章对2-苯基环丙胺及其衍生物的合成路线进行系统总结和概括,并对各路线进行简要评述。2-Phenylcyclopropylamine and its derivatives are important chiral pharmaceutical intermediates for antineoplastics,antidepressants and anticoagulants.The strategies for the synthesis of 2-phenylcyclopropylamine mainly include direct synthesis from cyclopropane-based derivatives and de novo construction of cyclopropane(CoreyChaykovsky reaction,Kulinkovich-de Meijere reaction,etc.).In this paper,synthetic routes of 2-phenylcyclopropylamine derivatives are systematically summarized and outlined,the advantages and disadvantages of each route are briefly reviewed.

关 键 词：2-苯基环丙胺类衍生物 药物分子 优势骨架 成药性 合成工艺 

分 类 号：TQ460.6[化学工程—制药化工] R914[医药卫生—药物化学]