摘要
A three-component cascade cyclization catalyzed by copperwas employedto synthesize quinoline-4-thiols using easily available diaryliodoniumsalts, alkynyl sulfides, and nitriles as starting materials. Sulfuratoms play an important role in controlling the regioselectivity,by stabilizing the high-valent vinyl copper intermediate. Meanwhile,the sulfide group at position 4 of quinoline could be further utilizedas a transformable group for ipso-transformationand as a directing group for C-H functionalization, affordingvarious multifunctional quinoline derivatives.