1. Office of Scientific Research, Anhui Provincial Institute for Food and Drug Control, Hefei 230022, China;2. School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China
Abstract:
A convenient and regioselective one-pot synthesis of 3-chloride or 3-bromide quinoline derivatives was achieved through a Grignard addition reaction by alkynyl Grignard regent to o-trifluoroacetyl aniline and a Cu(II)-catalyzed cyclization–halogenation tandem reaction with aqueous HCl or HBr as electrophilic reagent.