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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http://dx.doi.org/10.1021/ol402471y | DOI Listing |
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