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Copper/Guanidine‐Catalyzed Asymmetric Alkynylation of Isatins

Research paper by Quangang Chen, Yu Tang, Tianyu Huang, Prof. Dr. Xiaohua Liu, Dr. Lili Lin, Prof. Dr. Xiaoming Feng

Indexed on: 18 Mar '16Published on: 17 Mar '16Published in: Angewandte Chemie International Edition



Abstract

The highly enantioselective alkynylation of isatins, catalyzed by a bifunctional guanidine/CuI catalyst under mild reaction conditions, is described. The reaction is broad in scope with respect to alkyl/aryl‐substituted terminal alkynes and substituted isatins, thus affording bioactive propargylic alcohols in excellent yields and enantioselectivities.