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new steroidverbindungen, processes for their manufacture and their use

机译:新的甾类动词,其制造方法和用途

摘要

1409240 3α- Hydroxy-19-nov-5α-pregnane- 11,20-dione GLAXO LABORATORIES Ltd 8 Nov 1972 [11 Nov 1971] 52466/71 Heading C2U The novel title compound is prepared by sterospecific reduction of the corresponding 3-one, preferably by the method disclosed in Specification 1,409,239, or by hydrogenating the corresponding #SP16/SP-steroid. 19 - Nor - 5α- pregnane - 3,11,20 - trione is prepared by converting 11α,17α-dihydroxy-19- norpregn.-4-ene-3,20-dione to a semicarbazide and dehydrating and hydrolysing this to give 11α - hydroxy - 19 - norpregna - 4,16 - diene- 3,20 - dione, reducing this to 3#,11α,29#-trihydroxy - 19 - nor - 5α - pregnane and oxidizing this. 3α - Hydroxy 19 - nor - 5α - pregn. - 16- ene - 11,20 - dione is prepared by hydrogenating the same starting material to give 11α,- 17α - dihydroxy - 19 - nor - 5α - pregnane - 3,20 - diene, dehydrating this via a semicarbazide to 11α-hydroxy - 19-nor - 5α-pregn- 16-ene-3,20-dione, oxidizing this to 19 - nor - 5α - pregn - 16 - ene - 3,11,20 - trione and sterospecifically reducing this. The novel comound may be converted to 2#-substituted-5α-pregnanes via the corresponding 2α,3α-epoxy compound and to the corresponding 17#-carboxy-androstane and its esters by oxidation and, when desired, esterification. The novel steroid is stated to possess anaesthetic, hypnotic and sedative properties and it may be made up into pharmaceutical compositions with suitable carriers. Surface-active agents may be used to prepare aqueous injection solutions.
机译:14092403α-羟基-19-nov-5α-孕烯基11,20-二酮GLAXO LABORATORIES Ltd 1972年11月8日[1971年11月11日] 52466/71标题C2U通过对相应的3-one进行立体异构还原制备了新的标题化合物,优选通过说明书1,409,239中公开的方法,或通过氢化相应的# 16 -类固醇。 19-Nor-5α-孕烯-3,11,20-三烯酮是通过将11α,17α-二羟基-19-正孕烷-4-烯-3,20-二酮转化成氨基脲并脱水水解得到11α来制备的-羟基-19-正戊烷-4,16-二烯-3,20-二酮,将其还原为3#,11α,29#-三羟基-19-正-5α-孕烯并将其氧化。 3α-羟基19-也不-5α-妊娠通过将相同的原料氢化得到11α,-17-烯-11,20-二酮,得到11α,-17α-二羟基-19-也不-5α-孕烷-3,20-二烯,通过氨基脲将其脱水成11α-羟基-19-nor-5α-pregn-16-ene-3,20-dione,将其氧化为19-nor-5α-pregn-16-ene-3,11,20-trione并经立体定向还原。该新化合物可通过相应的2α,3α-环氧化合物转化为2#-取代的5α-孕烯,并通过氧化和在需要时通过酯化转化为相应的17#-羧基-雄甾烷及其酯。据称该新型类固醇具有麻醉,催眠和镇静作用,可以制成具有合适载体的药物组合物。表面活性剂可用于制备水性注射溶液。

著录项

  • 公开/公告号DE000002255153A

    专利类型

  • 公开/公告日1973-05-24

    原文格式PDF

  • 申请/专利权人 GLAXO LAB LTD;

    申请/专利号DE2255153A

  • 申请日1972-11-10

  • 分类号C07C169/34;

  • 国家 DE

  • 入库时间 2022-08-23 07:01:27

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