A method of bcr-abl inhibitor prepared intermediate

2014 
A method of BCR-ABL inhibitors Preparation of Intermediates. A process for preparing N- methyl-4- (4-nitro-2- (trifluoromethyl) phenyl) piperazine (Compound 4), comprising the steps of: 1) in a solvent, and the compound 1 had oxide halogenating agent and halogenation occurs, step 2) in a solvent, the resulting product of step 1 with N- methylpiperazine in the presence of a base and a phosphite prepared by reacting compound 4. The method of preparation of the present invention, the 2-trifluoromethyl-4-nitro-toluene (compound 1) as a raw material prepared by halogenation of 4-nitro-2-trifluoromethyl-benzyl halide (compound 2a) conversion more than 95%, based on the starting 2-trifluoromethyl-4-nitro-toluene (compound 1) count over two steps synthesis of compound 4 in a yield of 80% or more.
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