Formal α-trifluoromethylthiolation of carboxylic acid derivatives via N-acyl pyrazoles†
Abstract
Herein we disclosed a one-pot two-step protocol for the first direct, base-catalyzed α-trifluoromethylthiolation of carboxylic acid derivatives by using readily available N-acyl pyrazoles, N-(trifluoromethylthio)phthalimide and a nucleophile such as amines, alcohols and water. Straightforward elaboration of the products to alcohols and triflones expands further the synthetic utility of the process.
 
                




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