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

Add time:08/24/2019    Source:sciencedirect.com

In this paper, a one-step copper-catalyzed procedure for oxidative coupling of active methylene compounds including cyclic β-diketones, cyclic β-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 time via the process which is free from the foul smell of thiols.

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