Facile access to C-substituted piperazin-2-ones and mianserin derivative enabled by chemoselective carbene insertion and cyclization cascade

Abstract

The chemoselective N-H insertion of unsymmetrical diamines into carbene is a longstanding challenge. A simple copper-catalyzed strategy for synthesizing C-substituted piperazinones is described, employing easily accessible diazo compounds and 1,2-diamines....