A process for producing an alpha-acyloxy-alpha beta-unsaturated carbonyl compound and a 20-acyl-oxy-17(20)-methylen-21-al-steroid compound
    61.
    发明公开
    A process for producing an alpha-acyloxy-alpha beta-unsaturated carbonyl compound and a 20-acyl-oxy-17(20)-methylen-21-al-steroid compound 失效
    一种制备阿尔法 - 乙酰氧基 - 不饱和碳酸酯化合物的方法和20-乙酰氧基-17(20) - 甲基-21-AL-​​甾体化合物

    公开(公告)号:EP0306969A3

    公开(公告)日:1990-03-07

    申请号:EP88114770.6

    申请日:1988-09-09

    Abstract: There are disclosed a process for producing an α-acyloxy-α,β-unsaturated carbonyl compound represented by the general formula (VI):
    wherein Ri, R 2 and R4 are independently hydrogen atoms or substituted or unsubstituted hydrocarbon residues, or Ri, R 2 and R 4 , when taken together with one another in an optional combination, form a ring, R 3 is a substituted or unsubstituted hydrocarbon residue, and indicates that the configuration may be either E-configuration or Z-configuration, in particular, a 20-acyloxy-17(20)-methylen-21-al-steroid represented by the partial structural formula (II): wherein R is a hydrocarbon residue, and indicates that the configuration of the acyloxy group and the formyl group bonded to the carbon atom at the 20-position may be either E-configuration or Z-configuration, which comprises oxidizing a propargyl ester represented by the general formula (V):
    wherein Ri, R 2 , R 3 and R 4 have the same meanings as defined above; an al-steroid compound having the above partial structural formula which is an intermediate for producing a 21-acyloxy-20-keto-delta16-steroid being extremely useful as an intermediate for important corticoids as drugs and obtained by being subjected said al-steroid to isomerization reaction; and a process for producing a 21-acyloxy-20-keto- delta 16 -steroid which comprises oxidation reaction and isomerization reaction.

    17-Halogenmethylen-estratriene
    62.
    发明公开
    17-Halogenmethylen-estratriene 失效
    17 Halogenmethylen-雌三烯。

    公开(公告)号:EP0320438A1

    公开(公告)日:1989-06-14

    申请号:EP88730274.3

    申请日:1988-12-05

    CPC classification number: C07J13/007

    Abstract: 17-Halogenmethylen-estratriene der allgemeinen Formel I
    worin
    R₁ ein Wasserstoffatom, eine Methyl- oder Acylgruppe und
    R₂ ein Halogenatom
    bedeuten.
    Die Verbindungen zeigen geringe Affinität zum Östrogenrezeptor und bewirken eine im Vergleich mit Estradiol erhöhte Zellmembran- und Blut-/Lymphgefäßpermeabilität.

    Abstract translation: 其中R 1为氢原子,甲基或酰基,R 2为卤素原子的通式为I ... 的17-卤代亚甲基 - 亚甲基三烯。 ...与细胞膜和血液/淋巴管通透性中的雌二醇相比,化合物对雌激素受体的亲和力低。

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