STRAIGHTFORWARD TRIFLUOROACYLATION OF OXAZOLES – SCALABLE, COST-EFFECTIVE WAY TOWARD DIVERSE 2-(TRIFLUOROACETYL)OXAZOLES

Abstract

Feasible, scalable, and cost-effective method for the synthesis of low-molecular 2-(trifluoroacetyl)oxazoles from the corresponding oxazoles and trifluoroacetic anhydride was elaborated. The procedure was scaled up to 70 g of the desired ketones in a single run. Tolerance of the oxazole core to various functional group transformations was demonstrated. Thus, synthesis of various building blocks approved the possibility of using 2-(trifluoroacetyl)oxazoles as a starting materials for medicinal chemistry.