首页> 外国专利> Process for manufacture of {62 -(3-oxo-7 {60 -thioa cyl-17{62 -hydroxy-4-androstene-17{60 -yl) propionic acid {65 -lactones

Process for manufacture of {62 -(3-oxo-7 {60 -thioa cyl-17{62 -hydroxy-4-androstene-17{60 -yl) propionic acid {65 -lactones

机译:制备{62-(3-氧代-7 {60-硫代酰基-17 {62-羟基-4-雄烯基-17 {60-基))丙酸{65-内酯的方法

摘要

The present invention relates to an improved process for the manufacture of beta -(3-oxo-7 alpha -thioacyl-17 beta -hydroxy-4-androstene-17 alpha -yl)-propionic acid gamma -lactones in which a beta -(3-oxo-17 beta -hydroxy-4,6-androstadiene-17 gamma -yl)-propionaldehyde cyclohemiacetal alkyl glycoside is reacted with a thiocarboxylic acid in a mixture of water and an organic solvent miscible with water to yield a 3-(3'-oxo-7 alpha '-thioacyl-17 beta '-hydroxy-4'-androstene-17 alpha '-yl)-propionaldehyde cyclohemiacetal alkyl glycoside and in which the compound thus obtained is oxidized in an acid solution, the alkyl glycoside radical in the cyclohemiacetal group being split off, to yield the corresponding gamma -lactone; the invention further relates to new intermediates useful in this process and having the formula IN WHICH R1 stands for the methyl group or a hydrogen atom and R2 and R3 each for an alkyl group having 1 to 5 carbon atoms.
机译:本发明涉及一种制备β-(3-氧代-7α-硫代酰基-17β-羟基-4-雄烯基-17α-基)-丙酸γ-内酯的改进方法,其中β-(-在水和可与水混溶的有机溶剂的混合物中,将3-oxo-17 beta -hydroxy-4,6-androstadiene-17 gamma-yl)-丙醛环半缩醛烷基糖苷与硫代羧酸反应'-oxo-7α'-硫代酰基-17β'-羟基-4'-雄烯基-17α'-基)-丙醛环半缩醛烷基糖苷,其中所得化合物在酸性溶液中被氧化,烷基糖苷基团在环半缩醛基团被分离时,产生相应的γ-内酯;本发明进一步涉及在该方法中有用的并且具有式IN的新的中间体,其中R 1代表甲基或氢原子,R 2和R 3分别代表具有1-5个碳原子的烷基。

著录项

  • 公开/公告号US3894006A

    专利类型

  • 公开/公告日1975-07-08

    原文格式PDF

  • 申请/专利权人 HOECHST AKTIENGESELLSCHAFT;

    申请/专利号US19730403018

  • 发明设计人 STACHE;ULRICH;RADSCHEIT;KURT;

    申请日1973-10-03

  • 分类号C07C173/00;

  • 国家 US

  • 入库时间 2022-08-23 03:28:46

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