| 摘要 |
<p>The invention provides a novel process for the preparation of trifluoromethylacetophenones of general formula (I), wherein the position of the CF3-group on the aromatic ring may be in the 2- or 3-position relative to the acetyl, which process comprises (a) reacting a trifluoromethylbenzoyl halide of general formula (II), wherein the position of the CF3-group on the aromatic ring may be in the 2- or 3-position relative to the acetyl and Hal is a halogen atom selected from the group consisting of fluorine, chlorine, bromine, and iodine, with a cyclic secondary amine of general formula (III), wherein A is C3-C7-alkylene bridge which may be interrupted by a oxygen or sulfur atom in the presence of an aqueous base, used as an acid acceptor, resulting in the formation of a cycloalkyl-trifluoromethylbenzamide of general formula (IV), wherein the position of the CF3-group on the aromatic ring and A are as defined above, and (b) adding a methyl Grignard reagent to said cycloalkyl-trifluoromethylbenzamide followed by acidification with an aqueous acidification reagent to form the trifluoromethylacetophenone of formula (I).</p> |
