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PREPARATION METHOD OF AMOROLFINE HYDROCHLORIDE

机译:盐酸阿莫罗芬的制备方法

摘要

A preparation method of amorolfine hydrochloride comprises: with N-methylpyrrolidone as a solvent, in the presence of a palladium catalyst and a base, reacting 4-iodo-tert-amyl benzene with 2-methallyl alcohol, to obtain 3-tert-amylphenyl-2-methyl propionic acid; in the presence of glacial acetic acid, with triacetoxy sodium borohydride as a reducing agent, subjecting the obtained 3-tert-amylphenyl-2-methyl propionic acid and cis-2,6-dimethyl morpholine to reductive amination, to obtain amorolfine; and converting amorolfine into amorolfine hydrochloride.
机译:盐酸阿莫罗芬盐酸盐的制备方法包括:以N-甲基吡咯烷酮为溶剂,在钯催化剂和碱的存在下,使4-碘-叔戊基苯与2-甲基烯丙基醇反应,得到3-叔戊基苯基- 2-甲基丙酸;在冰醋酸的存在下,以三乙酰氧基硼氢化钠为还原剂,对所得的3-叔戊基苯基-2-甲基丙酸和顺式2,6-二甲基吗啉进行还原胺化反应,得到阿莫罗芬;并将阿莫罗芬转化为盐酸阿莫罗芬。

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