Angewandte Chemie. International edition in English 2012-01-09

Highly selective trifluoromethylation of 1,3-disubstituted arenes through iridium-catalyzed arene borylation.

Tianfei Liu, Xinxin Shao, Yaming Wu, Qilong Shen

Index: Angew. Chem. Int. Ed. Engl. 2nd ed., 51 , 540-543, (2012)

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Abstract

The old one two: A sequential iridium-catalyzed borylation and copper-catalyzed trifluoromethylation of arenes is described (see scheme; Pin = pinacol). The reaction is conducted under mild reaction conditions and tolerates a variety of functional groups. The advantages of this tandem procedure are demonstrated by the late-stage trifluoromethylation of a number of biologically active molecules.Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.