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Method for the synthesis of rilpivirine intermediate
Method for the synthesis of rilpivirine intermediate
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机译:利匹韦林中间体的合成方法
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摘要
Disclosed is process for the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amino-1-carboxybenzyl phenylamine (VI) with acrylonitrile in presence of palladium acetate, followed by treatment with an acid and its subsequent conversion to the hydrochloride salt (II), wherein the undesired Z isomer is less than 0.5% and provides Rilpivirine hydrochloride having Z isomer less than 0.1%.
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