K(2)CO(3)-promoted synthesis of amides from 1-aryl-2,2,2-trifluoroethanones and amines under mild conditions

在温和条件下,K₂CO₃促进1-芳基-2,2,2-三氟乙酮与胺合成酰胺

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Abstract

A base-promoted amidation of 1-aryl-2,2,2-trifluoroethanones with amines via Haller-Bauer reaction has been developed. In this reaction, the direct transformation of 1-aryl-2,2,2-trifluoroethanones into amides via C(O)-C bond cleavage occurs without the use of any stoichiometric chemical oxidants or transition-metal catalysts. A series of primary and secondary amines are shown to be compatible with this transformation, and several pharmaceutical molecules were synthesized.

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