Gold-Catalyzed Umpolung Sonogashira-Type Coupling of Boronic Acids with Alkynyl Iodine(III) Reagents

Abstract

A gold-catalyzed C(sp)–C(sp2) cross-coupling reaction between hypervalent iodine(III) reagents and boronic acids has been developed, enabling the efficient synthesis of alkyne derivatives. This methodology features a broad substrate scope, high functional-group tolerance, and proceeds under mild reaction conditions without requiring external base. Notably, the reaction is scalable to the gram-up level, and the resulting alkyne products can be readily transformed into structurally diverse derivatives.