CuI-catalyzed thioarylation of active methylene compounds with in situ generated benzenethiols: Preparation of α-thioaryl- β-dicarbonyls and 4-thioaryl-5-pyrazolones

摘要

In this paper, a one-step copper-catalyzed procedure for oxidative coupling of active methylene compounds including cyclicβ-diketones, cyclicβ-ketoesters and 5-pyrazolone with benzenethiols is described. Benzenethiols are in situ generated in the reaction mixture from aryl halides and thiourea as sulfur transfer reagent.α-Thioaryl compounds are obtained in excellent yields and in short reaction timeviathe process which is free from the foul smell of thiols.