Palladium-Catalyzed Amination of N-Free 2-Chloro-7-azaindole

Org Lett. 2015 Oct 2;17(19):4710-3. doi: 10.1021/acs.orglett.5b02173.

Abstract

A simple and efficient procedure for the Pd-catalyzed amination of N-free 2-chloro-7-azaindole is described, using either primary or secondary amines. An optimized combination of Brettphos, a Brettphos precatalyst, and LiHMDS in THF led us to a novel methodology, applied to various functionalized amines to study the scope of the reaction. This is the first report of cross-coupling amination on N-free 2-chloro-7-azaindole.

Publication types

  • Research Support, Non-U.S. Gov't