Formamidation of a wide range of substituted and functionalized amines with CO and a base

Abstract

Current methods for preparing formamides are limited by the narrow substrate scope and requirement for harsh reaction conditions. A base-mediated formamidation of amines with CO (<2 bar) under mild conditions was developed, which enabled the synthesis of a wide range of formamides in 61% to 98% yields under transition-metal-free conditions. This provides a useful strategy for generating gram amounts of various aromatic and aliphatic amides.