The synthesis of alk-2-ynl Weinreb amides via Pd/Cu-catalysed oxidative carbonylation of terminal alkynes

Abstract

Synthesis of alk-2-ynl-Weinreb amides via Pd-catalyzed oxidative carbonylation of terminal alkynes and N,O-dimethylhydroxylamine hydrochloride at room temperature under low CO/O₂ pressure is reported for the first time. This protocol offers tolerance of various functional groups under mild reaction conditions. The protocol incorporates aromatic- and aliphatic-substituted alkynes through a one-step oxidative carbonylative route toward desired alkynyl Weinreb amides, which are of considerable importance as valuable synthetic building blocks.