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Method for producing 4- (cyclopropylcarbonyl) -α, α-dimethylphenylacetic acid which is a high-purity pharmaceutical intermediate

机译:作为高纯度药物中间体的4-(环丙基羰基)-α,α-二甲基苯基乙酸的制造方法

摘要

This invention relates to a novel process to obtain highly pure 4-(cyclopropylcarbonyl)-alpha,alpha-dimethylphenylacetic acid of Formula I through crystallization from a mixture of para and meta regioisomers of Formula I and II in cyclohexane, whereby the amount of undesired meta isomer, 3-(cyclopropylcarbonyl)-alpha,alpha-dimethylphenylacetic acid of Formula II is decreased to below 0.5%. The compound of Formula I is a key intermediate for the preparation of high purity terfenadine carboxylate, which is a known antihistaminic.
机译:本发明涉及一种新颖的方法,该方法通过在环己烷中从式I和II的对位和间位异构体的混合物中结晶而获得高纯度的式I的4-(环丙基羰基)-α,α-二甲基苯基乙酸,由此得到不希望的间位式II的异构体3-(环丙基羰基)-α,α-二甲基苯基乙酸降低到0.5%以下。式I化合物是制备高纯度特非那定羧酸盐的关键中间体,其是已知的抗组胺药。

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