15 Hydroxylation of 1.alpha.,2.alpha.-methylene steroids
    2.
    发明授权
    15 Hydroxylation of 1.alpha.,2.alpha.-methylene steroids 失效
    15个α,2个α-亚甲基类固醇的羟基化

    公开(公告)号:US4337311A

    公开(公告)日:1982-06-29

    申请号:US96349

    申请日:1979-11-21

    CPC分类号: C07J53/005

    摘要: Steroids of the formula ##STR1## wherein R.sub.1 and R.sub.2 are identical or different and each is hydrogen or the residue of an organic or inorganic acid,and for the esters (R.sub.1 or R.sub.2 is not H) capable of salt formation, the salts thereof, possess valuable pharmacoligical properties, e.g., good antiandrogenic activity with low progestational activity.

    摘要翻译: 其中R1和R2相同或不同,并且各自为氢或有机酸或无机酸的残基,并且对于能够形成盐的酯(R 1或R 2不是H),其盐, 具有宝贵的药理学性质,例如良好的抗雄激素活性,具有较低的孕激素活性。

    Novel .alpha.-hydroxy steroids
    5.
    发明授权
    Novel .alpha.-hydroxy steroids 失效
    新型{60-羟基类固醇

    公开(公告)号:US4144334A

    公开(公告)日:1979-03-13

    申请号:US767420

    申请日:1977-02-10

    摘要: 1.alpha.-Oxysteroid of the formula ##STR1## wherein R.sub.1 is methyl or ethyl,R.sub.2 and R.sub.3 each are hydrogen or alkanoyl of 1-8 carbon atoms, andR.sub.4 is hydrogen or hydrocarbon of 1-4 carbon atoms,Are progestestionally active and useful in oral contraceptive and menopausal compositions.

    摘要翻译: 1α-类型的化学式其中R 1是甲基或乙基,R 2和R 3各自是氢或碳原子的烷酰基,且R 4是氢或1-4个碳原子的烃,ARE PROGESTESTIONALLY ACTIVE AND USEFUL 口服合同和男性组成。

    Novel agents and novel methods for inducing abortions
    6.
    发明授权
    Novel agents and novel methods for inducing abortions 失效
    用于诱导堕胎的新型药剂和新方法

    公开(公告)号:US4124708A

    公开(公告)日:1978-11-07

    申请号:US781275

    申请日:1977-03-25

    IPC分类号: C07J1/00 A61K31/56

    CPC分类号: C07J1/0096 C07J1/007

    摘要: Novel agents and methods for triggering abortions employ a compound of the formula ##STR1## wherein R.sub.1 is methyl or ethyl, R.sub.2 and R.sub.3 are hydrogen or alkanoyl of 1-8 carbon atoms, and R.sub.4 is hydrogen or ethynyl.

    摘要翻译: 用于触发流产的新型药剂和方法使用下式的化合物,其中R 1是甲基或乙基,R 2和R 3是氢或1-8个碳原子的烷酰基,R 4是氢或乙炔基。

    Racemic dissociation of 3-acyloxy bicyclo(3.3.0)octan-7-one-2-carboxylic
acid esters by stereospecific enzymatic or microbiological acylate
hydrolysis
    9.
    发明授权
    Racemic dissociation of 3-acyloxy bicyclo(3.3.0)octan-7-one-2-carboxylic acid esters by stereospecific enzymatic or microbiological acylate hydrolysis 失效
    3-立体特异性酶或微生物酰化物水解3-酰氧基双环(3.3.0)辛-7-酮-2-羧酸酯的外消旋解离

    公开(公告)号:US4894336A

    公开(公告)日:1990-01-16

    申请号:US237109

    申请日:1988-07-13

    摘要: Process for the production of optically active (+)-bicyclo[3.3.0]octanol derivatives of formula (+)-I, in which R.sub.1 and R.sub.2 represent jointly an oxygen atom or the double-bond residue --O--X--O-- with X as a straight or branched-chain alkylene with 1-7 C-atoms, or R.sub.1 and R.sub.2 represent separately the residue OR.sub.5 with R.sub.5 as a straight or branched-chain alkyl with 1-7 C-atoms, and R.sub.3 the residue COOZ with Z as a hydrogen atom, straight or branched chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 atoms or R.sub.3 is the residue --(CH.sub.2).sub.n --O--COR.sub.4 with n having the meaning 1-4 and R.sub.4 as a straight or branched-chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 C atoms. The process is characterized in that racemic 3.alpha.-cyloxy-cis-bicyclo[3.3.0]-octane derivatives of formula (+)-II, wherein R.sub.1, R.sub.2 R.sub.3 and R.sub.4 have the above meanings, are subjected enzymatically or microbiologically to a stereospecific acylate hydrolsis and the (+)-bicyclo[3.3.0]-octanol derivative produced is separated from the unsaponified bicyclo[3.3.0]-octanol acylate of formula (-)-II or the unsaponified enantiomers (+)-II are separated from the saponified bicyclo[3.3.0]octanol derivative (-)-I and then subjected to chemical acylate hydrolysis.

    摘要翻译: PCT No.PCT / DE87 / 00513 Sec。 371日期:1988年7月13日 102(e)日期1988年7月13日PCT提交1987年11月12日PCT公布。 出版物WO88 / 03567 日期:1988年5月19日。制备式(+) - I的光学活性(+) - 双环[3.3.0]辛醇衍生物的方法,其中R 1和R 2共同表示氧原子或双键残基-OXO - X为具有1-7个C原子的直链或支链亚烷基,或者R1和R2分别表示残基OR5与R5作为具有1-7个C原子的直链或支链烷基,R3表示残基 具有Z作为氢原子的COOZ,具有1-7个C原子的直链或支链烷基,具有3-6个C原子的环烷基,具有7-10个原子的苯基或芳烷基或R3是残基 - (CH2)nO-COR4,其中n 具有1-4和R4为具有1-7个C原子的直链或支链烷基,具有3-6个C原子的环烷基,具有7-10个C原子的苯基或芳烷基。 该方法的特征在于其中R1,R2R3和R4具有上述含义的式(+) - II的外消旋3α-甲氧基 - 顺式 - 双 - 二环[3.3.0] - 辛烷衍生物经酶促或微生物方式进行立体特异性 将酰化物水解和(+) - 双环[3.3.0] - 辛醇衍生物与式( - ) - II的未皂化的双环[3.3.0] - 辛醇酰化物分离,或未分离的对映异构体(+) - 从皂化的双环[3.3.0]辛醇衍生物( - ) - I中,然后进行化学酰化物水解。