title: Synthesis of quinazolin-4(3H)-ones via Pd(II)-catalyzed intramolecular C(sp2)-H carboxamidation of N-arylamidines.
abstract: An efficient synthesis of quinazolin-4(3H)-ones from N-arylamidines, through palladium-catalyzed intramolecular C(sp(2))-H carboxamidation, has been developed. The reaction, carried out in the presence of 1.0 equiv of CuO as oxidant under atmospheric pressure of CO, provides diversified 2-aryl(alkyl)quinazolin-4(3H)-ones in reasonable to good yields from N-arylamidines, which are readily derived from anilines and nitriles. Compared with existing approaches to quinazolin-4(3H)-ones, the current strategy features atom-economy and step-efficiency.
authors.affiliation: State Key Laboratory of Respiratory Disease, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, 190 Kaiyuan Avenue, Guangzhou 510530, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Ma
authors.forename: Yong
authors.initials: Y
authors.lastname: Wang
authors.forename: Jiangling
authors.initials: J
authors.lastname: Peng
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhu
mesh_terms: D000578:Amidines / Q000737:chemistry*; D000814:Aniline Compounds / Q000737:chemistry*; D002384:Catalysis; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009570:Nitriles / Q000737:chemistry*; D010165:Palladium / Q000737:chemistry*; D052999:Quinazolinones / Q000138:chemical synthesis* / Q000737:chemistry*; D013237:Stereoisomerism
chemical_list: D000578:Amidines; D000814:Aniline Compounds; D009570:Nitriles; D052999:Quinazolinones; D010165:Palladium