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 and high functional-group tolerance, and proceeds under mild reaction conditions without requiring external bases. Notably, the reaction is scalable to the gram level, and the resulting alkyne products can be readily transformed into structurally diverse derivatives.