首页> 外国专利> method for preparing a medicine with effects on the central nervous system; method for preparation of a medicinal compound which is suitable to be used;therapeutic agent.

method for preparing a medicine with effects on the central nervous system; method for preparation of a medicinal compound which is suitable to be used;therapeutic agent.

机译:制备对中枢神经系统有影响的药物的方法;适于使用的药物化合物的制备方法;治疗剂。

摘要

1436821 4 - Hydroxy - 2,9 - dioxatricyclo [4,3,1,0SP3,7/SP]decanes KALI-CHEMIE PHARMA GmbH 18 Jan 1974 [8 Feb 1973] 02548/74 Heading C2C Novel compounds I in which R 1 is C 1-4 alkyl, R 2 is OCOR 4 or OCONHR 5 when R 3 is hydrogen and R 3 is OCONHR 5 when R 2 is hydrogen (R 4 is C 1-4 alkyl and R 5 is a C 1-6 alkyl, C 2-6 unsaturated aliphatic, C 3-6 cycloaliphatic or aromatic group) and the 10,11 bond may be hydrogenated are prepared by reducing a compound III in which the 10,11 bond may be hydrogenated preferably with a metal hydride to form a mixture of the corresponding 4- and 4#- hydroxy compounds and reacting the 4-OH compound with a carboxylic acid chloride R 4 COCl, a carboxylic anhydride (R 4 CO) 2 O, an isocyanate R 5 NCO, an ester or chloride of a carbamic acid R 5 NH-COR 6 (in which R 6 is chlorine or alkoxy) or with phosgene followed by an amine R 5 NH 2 to form compounds I (R 3 =H): compounds I (R 3 = OCONHR 5 ) are prepared from the corresponding 4#-hydroxy compound by the methods described above. Compounds I have sedative, hyprotic and narcotic properties and may be administered orally or parenterally.
机译:1436821 4-羟基-2,9-二氧三环[4,3,1,0 3,7 ]癸烷KALI-CHEMIE PHARMA GmbH 1974年1月18日[1973年2月8日] 02548/74标题C2C新化合物式I,其中R 1是C 1-4烷基,当R 3是氢时,R 2是OCOR 4或OCONHR 5,而当R 2是氢时,R 3是OCONHR 5(R 4是C 1-4烷基,R 5是a C 1-6烷基,C 2-6不饱和脂肪族,C 3-6脂环族或芳族基团和可以氢化的10,11键是通过还原化合物III制备的,其中优选将10,11键氢化金属氢化物形成相应的4-和4#-羟基化合物的混合物,并使4-OH化合物与羧酸氯化物R 4 COCl,羧酸酐(R 4 CO)2 O,异氰酸酯R 5 NCO反应,氨基甲酸酯R 5 NH-COR 6(其中R 6为氯或烷氧基)或与光气的酯或氯化物,然后与胺R 5 NH 2形成化合物I(R 3 = H):化合物I( R 3 = OCONHR 5)由相应的4制备通过上述方法得到#-羟基化合物。化合物I具有镇静,促质和麻醉作用,可以口服或胃肠外给药。

著录项

  • 公开/公告号NL183011B

    专利类型

  • 公开/公告日1988-02-01

    原文格式PDF

  • 申请/专利号NL19740000404

  • 发明设计人

    申请日1974-01-11

  • 分类号A61K31/35;C07D493/00;

  • 国家 NL

  • 入库时间 2022-08-22 06:59:43

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