Pd/PTABS: Catalyst for Room Temperature Amination of Heteroarenes

Org Lett. 2018 Jan 19;20(2):473-476. doi: 10.1021/acs.orglett.7b03854. Epub 2018 Jan 5.

Abstract

A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields.

Publication types

  • Research Support, Non-U.S. Gov't