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7 条记录 (耗时 0.021 秒)

    Protected derivatives of the enone of spectinomycin
    1.
    发明授权
    Protected derivatives of the enone of spectinomycin 失效
    受保护的壮观霉素的衍生物

    公开(公告)号：US5220034A

    公开(公告)日：1993-06-15

    申请号：US847496

    申请日：1992-03-13

    申请人： Paul M. Herrinton

    发明人： Paul M. Herrinton

    IPC分类号： C07D493/04 ,  C07D497/04

    CPC分类号： C07D493/04 ,  C07D497/04

    摘要： Process for alkylating protected spectinomycin enone derivatives in the gamma position in order to produce intermediates useful in the synthesis of 6'alkylspectinomycins. The intermediate have the formula ##STR1## which comprises reacting a compound having the formula ##STR2## with a strong base and an alkenyl halide, wherein R.sub.1 is selected from the group consisting of alkoxycarbonyl, halogenated alkoxycarbonyl, aralkoxycarbonyl, and arylsulfone; R.sub.2 is selected from the group consisting of hydrogen, trimethylsilyl (TMS), tetrahydropyran (THP), and triethylsilyl (TES); A is selected from the group consisting of oxygen and sulfur; M is selected from the group consisting of lithium and potassium; and n is an integer from 1 to 3.

    摘要翻译： 用于在γ位置烷基化保护的壮观霉素烯酮衍生物以产生可用于合成6'-烷基保护霉素的中间体的方法。 中间体具有式III的化合物，其包括使具有式V的化合物与强碱和烯基卤反应，其中R 1选自烷氧基羰基，卤代烷氧基羰基，芳烷氧基羰基和芳基砜; R2选自氢，三甲基甲硅烷基（TMS），四氢吡喃（THP）和三乙基甲硅烷基（TES）; A选自氧和硫; M选自锂和钾; n为1〜3的整数。

    Oxidative preparation of 3,5-secoandrost-5-one-3,17 .beta.-dioic acid
    7.
    发明授权
    Oxidative preparation of 3,5-secoandrost-5-one-3,17 .beta.-dioic acid 失效
    3,5-二雄甾-5-酮-3,17β-二酸的氧化制备

    公开(公告)号：US5405978A

    公开(公告)日：1995-04-11

    申请号：US158174

    申请日：1993-11-24

    申请人： Paul M. Herrinton

    发明人： Paul M. Herrinton

    IPC分类号： C07C62/24 ,  C07C62/26 ,  C07D303/31 ,  C07J71/00 ,  C07J73/00 ,  C07C61/135

    CPC分类号： C07C62/26 ,  C07C62/24 ,  C07J71/0015 ,  C07J73/005

    摘要： The present invention is an oxidative process for the conversion of 21-unsaturated progesterones (I) ##STR1## to the corresponding 3,5-secoandrost-5-one-3,17.beta.-dioic acids (II) ##STR2## by use of either ozone or an oxidizing agent, which are useful intermediates in the production of .DELTA..sup.5 -4-aza-17-carbonyl steroids (III) which are useful in production of 5.alpha.-4-aza amide (IV) pharmaceuticals. Also disclosed are the novel 21-unsaturated progesterones (I-C) and 3,5-secoandrost-5-one-3,17.beta.-dioic acids (II-C).

    摘要翻译： 本发明是通过使用臭氧或氧化剂转化21-不饱和孕酮（I）罗哌酮-5-一-3,17β-二酸（II）（II）的氧化方法， 它们是生产可用于制备5α-4-氮杂酰胺（IV）药物的DELTA 5-4-氮杂-17-羰基类固醇（III）的有用的中间体。 还公开了新型的21-不饱和孕酮（I-C）和3,5-二雄甾-5-酮-3,17β-二酸（II-C）。