A Facile and Efficient One‐Pot Synthesis of Substituted Quinolines from α‐Arylamino Ketones Under Vilsmeier Conditions

Abstract

AbstractAn efficient one‐pot synthesis of substituted quinolines from α‐arylamino ketones in the presence of PBr3 in DMF has been developed. This general protocol provides a novel and facile access to substituted quinolines by sequential Vilsmeier–Haack reaction, intramolecular cyclization and aromatization reactions of α‐arylamino ketones. PBr3 plays a dual role in the quinoline synthesis: as a key component of the Vilsmeier reagent (PBr3/DMF) and as a reducing reagent. (© Wiley‐VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009)