Hypervalent iodine-mediated highly mono- and di-selective etherification of 8-aminoquinolines at the C5 and C6 positions

Abstract

A mild, metal-free and highly regioselective approach for etherification of 8-aminoquinoline scaffolds at their C5 and C6 positions has been developed with hypervalent iodine compounds. The transformation proceeds by direct C–H functionalization under mild reaction conditions employing various alcohols, including primary and secondary alcohols, and allyl, propargylic, and benzylic alcohols as effective coupling partners.