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Androstanol and androstenol derivatives

机译:雄甾烷醇和雄甾烯醇衍生物

摘要

The invention comprises compounds of the formula FORM:0948879/C2/1 and non toxic and quaternary salts thereof wherein A is a hydrogen atom or an alkanoyl radical containing 1 to 6 carbon atoms, R is a hydrogen atom or an alkyl radical containing 1 to 6 carbon atoms; Alk is an alkylene radical containing 2 to 5 carbon atoms which separates the R-N and Z functions by at least two carbon atoms; the dotted line indicates the optional presence of a double bonded linkage between carbon atoms 5 and 6; and Z is a radical of the general formula: -NR1R11 or the general formula FORM:0948879/C2/2 wherein R1 and R11 are each a hydrogen atom or, an alkyl radical containing 1 to 6 carbon atoms; L is methylene, epoxy or methylimino and n is O or 1. Such compounds may be prepared (a) by treating a 17-ketone with an amino-alkylamine and reducing the resultant imino compound (b) reacting a 17-ketone with an amino-alkylamine and formic acid and hydrolysing or reducing the resultant 17b -[N-(amino-alkyl) formamido] derivative; (c) alkylating a 17-ketone with a formamide of the formula H-CO-NH-R, hydrolysing the formamido compound thus formed, reacting the resultant amino compound with an a ,b -olefinic nitrile to obtain the corresponding N-(b -cyanoalkyl) amino derivatives which are reduced; (d) reacting a 17-amino compound with a haloalkanoyl halide to obtain a 17-haloalkyl-mido 3-haloalkyl ester, and reacting this compound with a primary amine to obtain a monoalkylaminoalkylamido compound which is reduced.
机译:本发明包括式的化合物及其无毒和季铵盐,其中A是氢原子或含有1-6个碳原子的烷酰基,R是氢原子或含有1至6个碳原子; Alk是含有2至5个碳原子的亚烷基,其通过至少两个碳原子分隔R-N和Z官能团;虚线表示在碳原子5和6之间任选存在双键。 Z为通式-NR1R11或通式的基团,其中R1和R11分别为氢原子或含1至6个碳原子的烷基。 L为亚甲基,环氧或甲基亚氨基,n为O或1。可以通过(a)通过用氨基烷基胺处理17-酮并还原所得的亚氨基化合物(b)使17-酮与氨基反应来制备此类化合物。 -烷基胺和甲酸,水解或还原所得的17b-[N-(氨基-烷基)甲酰胺基]衍生物; (c)用式H-CO-NH-R的甲酰胺烷基化17-酮,水解由此形成的甲酰胺基化合物,使所得的氨基化合物与α,b-烯烃腈反应,得到相应的N-(b -氰基烷基)被还原的氨基衍生物; (d)使17-氨基化合物与卤代烷酰基卤反应,得到17-卤代烷基-氨基3-卤代烷基酯,并使该化合物与伯胺反应,得到还原的单烷基氨基烷基酰胺基化合物。

著录项

  • 公开/公告号GB948879A

    专利类型

  • 公开/公告日1964-02-05

    原文格式PDF

  • 申请/专利权人 G. D. SEARLE & CO.;

    申请/专利号GB19620011672

  • 发明设计人

    申请日1962-03-27

  • 分类号C07C;

  • 国家 GB

  • 入库时间 2022-08-23 16:19:19

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