Pd(II)-catalyzed ortho-trifluoromethylation of benzylamines.

Org Lett

Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, United States.

Published: October 2013

AI Article Synopsis

  • Pd(II) catalyzes the ortho-C-H trifluoromethylation of benzylamines using an electrophilic CF3 reagent.
  • Key additives like H2O and Ag2O are essential for achieving high yields in this reaction.
  • This method is significant for medicinal chemistry, particularly for creating ortho-trifluoromethyl-substituted benzylamines.

Article Abstract

The Pd(II)-catalyzed ortho-C-H trifluoromethylation of benzylamines has been achieved utilizing an electrophilic CF3 reagent. Additives, such as H2O and Ag2O, were found to be crucial for obtaining good yields. This protocol will be useful in medicinal chemistry for the preparation of ortho-trifluoromethyl-substituted benzylamines.

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Source
http://dx.doi.org/10.1021/ol402471yDOI Listing

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