Palladium-Catalyzed Direct C-H Carbonylation of Free Primary Benzylamines: A Synthesis of Benzolactams

Org Lett. 2018 May 4;20(9):2595-2598. doi: 10.1021/acs.orglett.8b00786. Epub 2018 Apr 23.

Abstract

A protocol for palladium-catalyzed C-H carbonylation of readily available free primary benzylamines using NH2 as the chelating group under an atmospheric pressure of CO has been achieved, providing a general, atom- and step-economic approach to benzolactams, an important structural motif found in many biologically active compounds. Application of this new method is also exemplified in the concise syntheses of two bioactive molecules.

Publication types

  • Research Support, Non-U.S. Gov't