Amidation of unactivated ester derivatives mediated by trifluoroethanol

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Catalytic amidation of unactivated ester derivatives mediated by trifluoroethanol.

A catalytic amidation method has been developed, employing 2,2,2-trifluoroethanol to facilitate condensation of unactivated esters and amines, enabling the synthesis of a range of amide products in good to excellent yields. Mechanistic studies indicate the reaction proceeds through a trifluoroethanol-derived active ester intermediate.

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Amidation of unactivated ester derivatives mediated by trifluoroethanol.

A catalytic amidation protocol mediated by 2,2,2-trifluoroethanol has been developed, facilitating the condensation of unactivated esters and amines, furnishing both secondary and tertiary amides. The complete scope and limitations of the method are described, along with modified conditions for challenging substrates such as acyclic secondary amines and chiral esters with retention of chiral in...

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ژورنال

عنوان ژورنال: Organic & Biomolecular Chemistry

سال: 2017

ISSN: 1477-0520,1477-0539

DOI: 10.1039/c7ob00593h