首页> 外国专利> CONVERSION OF E ISOMER OF 1,2-DIPHENYL-1- (4-(2-DIMETHYLAMINOETHOXY)PHENYL)-1-BUTENE TO TAMOXIPHENE HCL

CONVERSION OF E ISOMER OF 1,2-DIPHENYL-1- (4-(2-DIMETHYLAMINOETHOXY)PHENYL)-1-BUTENE TO TAMOXIPHENE HCL

机译:1,2-二苯基-1-(4-(2-二甲基氨基乙氧基)苯基)-1-丁烯的电子异构体向盐酸三苯氧胺的转化

摘要

There is disclosed a process wherein the E isomer of 1,2-diphenyl-1-[4-(2-dimethylaminoethoxy) phenyl]-1-butene is converted to tamoxifen hydrochloride by a process which comprises heating the E isomer of 1,2-diphenyl-1-[4-(2-dimethylaminoethoxy) phenyl]-1-butene, either alone or in admixture with tamoxifen, in hydrochloric acid at a temperature within the range of 35-60 DEG C until substantial conversion of 1,2-diphenyl-1-[4-(2-dimethylaminoethoxy)-phenyl]-1-butene to tamoxifen is accomplished. In this temperature range, i.e., 35-60 DEG C the tamoxifen precipitates from the reaction mixture as the HC1 salt while most of the HC1 salt of the E isomer of 1,2-diphenyl-1-[4-(2-dimethylaminoethoxy)phenyl]-1-butene stays in solution. The tamoxifen HC1 is recovered from the resultant slurry. It can be further purified by conventional procedures, e.g., by chromatography or fractional crystallization.
机译:公开了一种方法,其中通过加热包括1,2的E异构体的方法将1,2-二苯基-1- [4-(2-二甲基氨基乙氧基)苯基] -1-丁烯的E异构体转化为盐酸他莫昔芬。 -二苯基-1- [4-(2-二甲基氨基乙氧基)苯基] -1-丁烯,单独或与他莫昔芬混合,在盐酸中于35-60℃的温度范围内直至基本上转化为1,2完成了对他莫昔芬的-二苯基-1- [4-(2-二甲基氨基乙氧基)-苯基] -1-丁烯。在此温度范围内,即35-60℃,他莫昔芬以HCl盐形式从反应混合物中沉淀出来,而大部分的HCl盐是1,2-二苯基-1- [4-(2-二甲基氨基乙氧基)的E异构体苯基] -1-丁烯保留在溶液中。从所得浆液中回收他莫昔芬HCl。可以通过常规方法,例如通过色谱法或分步结晶法进一步纯化。

著录项

  • 公开/公告号JPH0475224B2

    专利类型

  • 公开/公告日1992-11-30

    原文格式PDF

  • 申请/专利权人

    申请/专利号JP19840103784

  • 发明设计人

    申请日1984-05-24

  • 分类号C07C93/06;

  • 国家 JP

  • 入库时间 2022-08-22 05:12:56

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