title: ZrCl4-mediated regio- and chemoselective Friedel-Crafts acylation of indole.
abstract: An efficient method for regio- and chemoselective Friedel-Crafts acylation of indole using acyl chlorides in the presence of ZrCl(4) has been discovered. It minimizes/eliminates common competing reactions that occur due to high and multiatom-nucleophilic character of indole. In this method, a wide range of aroyl, heteroaroyl alkenoyl, and alkanoyl chlorides undergo smooth acylation with various indoles without NH protection and afford 3-acylindoles in good to high yields.
authors.affiliation: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), S A S Nagar (Mohali), Punjab, India. skguchhait@niper.ac.in
authors.forename: Sankar K
authors.initials: SK
authors.lastname: Guchhait
authors.forename: Maneesh
authors.initials: M
authors.lastname: Kashyap
authors.forename: Harshad
authors.initials: H
authors.lastname: Kamble
mesh_terms: D000215:Acylation; D002384:Catalysis; D002712:Chlorides / Q000737:chemistry*; D007211:Indoles / Q000737:chemistry*; D013237:Stereoisomerism; D013379:Substrate Specificity; D017967:Zinc Compounds / Q000737:chemistry*
chemical_list: D002712:Chlorides; D007211:Indoles; D017967:Zinc Compounds; C016837:zinc chloride