title: Synthesis of 3-Substituted 2-Arylpyridines via Cu/Pd-Catalyzed Decarboxylative Cross-Coupling of Picolinic Acids with (Hetero)Aryl Halides.
abstract: A decarboxylative cross-coupling of 3-substituted picolinic acids with (hetero)aryl halides is presented. In the presence of catalytic Cu2O and Pd(1,5-cyclooctadiene)Cl2with 2-dicyclohexylphosphino-2'-(N,N-dimethylamino)biphenyl as the ligand, both electron-rich and electron-deficient aryl bromides and chlorides as well as heteroaryl bromides were successfully coupled with various picolinate salts under mild conditions in yields up to 96%. This protocol provides an efficient entry to 2-(hetero)arylpyridines, an attractive substance class in drug discovery.
authors.affiliation: Fakultät für Chemie und Biochemie, Ruhr Universität Bochum , Universitätsstr. 150, 44801 Bochum, Germany.
authors.forename: Dagmar
authors.initials: D
authors.lastname: Hackenberger
authors.affiliation: Fakultät für Chemie und Biochemie, Ruhr Universität Bochum , Universitätsstr. 150, 44801 Bochum, Germany.
authors.forename: Philip
authors.initials: P
authors.lastname: Weber
authors.affiliation: Pfizer Inc. , Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: David C
authors.initials: DC
authors.lastname: Blakemore
authors.affiliation: Fakultät für Chemie und Biochemie, Ruhr Universität Bochum , Universitätsstr. 150, 44801 Bochum, Germany.
authors.forename: Lukas J
authors.identifier: 0000-0002-2547-3037
authors.initials: LJ
authors.lastname: Goossen