title: Brønsted acid promoted addition-cyclization and C-C bond cleavage: a convenient synthesis of 2-amino-5-aroylmethylthiazoles derivatives.
abstract: A Brønsted acid promoted C-C bond cleavage method for the synthesis of novel 2-amino-5-aroylmethylthiazole derivatives has been directly developed from 1,4-enediones and thioureas through self-sequenced thio-Michael-addition, intramolecular selective cyclization, dehydration/aromatization, and C-C bond cleavage reactions. It is noteworthy that this reaction has significant advantages in simple reagents, under environmentally benign conditions and with excellent yields. This highly efficient method is also a highly attractive alternative for the preparation of PLTP, CETP inhibitors and novel biheterocycles.
authors.affiliation: Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan Hubei 430079, China. chwuax@mail.ccnu.edu.cn.
authors.forename: Fan
authors.initials: F
authors.lastname: Ni
authors.forename: Yan
authors.initials: Y
authors.lastname: Yang
authors.forename: Wen-Ming
authors.initials: WM
authors.lastname: Shu
authors.forename: Jun-Rui
authors.initials: JR
authors.lastname: Ma
authors.forename: An-Xin
authors.initials: AX
authors.lastname: Wu