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    PREPARATION OF ESTER DERIVATIVES OF STEROIDS
    1.
    发明公开
    PREPARATION OF ESTER DERIVATIVES OF STEROIDS 失效
    DARSTELLUNG VON ESTERDERIVATEN VON STEROIDEN

    公开(公告)号：EP0866798A4

    公开(公告)日：1998-12-02

    申请号：EP96912447

    申请日：1996-03-20

    申请人： POPULATION COUNCIL INC

    发明人： LI FANG

    IPC分类号： C07J7/00 ,  C07J5/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J75/00

    CPC分类号： C07J7/0055

    摘要： The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17 alpha -hydroxy-19-norpregn-4-ene-3,20-dione.

    摘要翻译： 本发明涉及一种使用高氯酸催化反应制备去甲孕酮化合物，特别是16-亚甲基-17α-羟基-19-降孕-4-烯-3,20-二酮的酰基衍生物的方法。

    Nouveau procédé de préparation d'un stéroide 16bêta-méthyl et nouveaux intermédiaires
    2.
    发明公开
    Nouveau procédé de préparation d'un stéroide 16bêta-méthyl et nouveaux intermédiaires 失效
    对于它们的16-β-甾族化合物和新的中间体的制备新方法。

    公开(公告)号：EP0685487A1

    公开(公告)日：1995-12-06

    申请号：EP95401273.8

    申请日：1995-06-01

    申请人： ROUSSEL-UCLAF

    发明人： Geurts, Catherine ,  Vivat, Michel

    IPC分类号： C07J7/00 ,  C07J41/00 ,  C07J21/00 ,  C07J71/00

    CPC分类号： C07J13/005 ,  C07J7/0055 ,  C07J21/006 ,  C07J41/0094 ,  C07J71/001 ,  Y02P20/55

    摘要： L'invention concerne la préparation d'un intermédiaire de bétamétasone de formule (I) :

    au départ de la cyanhydrine de formule (II) :

    dans laquelle les cycles A et B représentent :

    ou

    où K est un radical oxo ou un groupe protecteur du radical oxo et R₁ un reste éther ou ester, ainsi que des intermédiaires nouveaux.

    摘要翻译： Prodn。 的16β-甲基-17阿尔法 - 羟基-4,9（11）式（I）的-pregnadiene -3,20-二酮包括：（a）治疗17的α-羟基 - 17的β腈与脱水剂 以得到16,17-脱氢-17-腈; （B）保护氧代GP。 如果必要的; （C）与有机金属甲基化试剂和水解所得亚胺，得到甲基酮反应; （D）在碱性介质中与环氧化剂处理，得到16α，17个阿尔法环氧化物; （E）保护20氧代GP。 （F）与有机金属甲基化试剂反应，得到一个16的β - 甲基DERIV; 及（g）脱保护氧代GPS。 给（我）。

    Steroidal esters and process for the preparation of steroidal esters
    6.
    发明公开
    Steroidal esters and process for the preparation of steroidal esters 失效
    类固醇酯和类固醇酯的制备方法。

    公开(公告)号：EP0072200A2

    公开(公告)日：1983-02-16

    申请号：EP82304116.5

    申请日：1982-08-04

    申请人： PLURICHEMIE ANSTALT

    发明人： Page, Philip Ronald Rua dos Girassois, Lote 38A ,  Heggie, William

    IPC分类号： C07J5/00 ,  C07J7/00 ,  A61K31/57

    CPC分类号： C07J5/0053 ,  C07J5/0076 ,  C07J7/0055 ,  C07J7/0085

    摘要： A process for the preparation of corticosteroid esters of the formula
    wherein

    --- signifies that a double bond can be present;
    X is hydrogen, fluorine or chlorine;
    R 1 is hydrogen, fluorine, chlorine or methyl, which may be either a or β;
    R 2 is halogen, oxo, i.e. ketonic oxygen, or hydroxyl;
    R 3 is hydrogen, a-methyl or β-methyl;
    R 4 is an acyl group of the formula RCO, in which R is one of the following:

    i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;
    ii) an aralkyl group of 7 to 8 carbon atoms; or
    iii) a phenyl group;

    R 5 is hydroxyl or R 6 ; where
    R 6 is hydrogen, halogen, two halogen atom substituents or
    OR 7 , where R 7 is an acyl group of the formula R'CO in which
    R', which can be identical or different to R in the same molecule, is one of the following:

    i) an alkyl group containing 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;
    ii) an aralkyl group of 7 to 8 carbon atoms; or
    iii) a phenyl group;

    which comprises esterifying a compound of the formula
    wherein X, R 1 , R 3 and R 5 are as defined above, and
    R 8 is trihaloacetate, halogen or oxo;
    at the 17-position only, or at the 17-and 21-positions when R 5 , in formula III, is hydroxyl, the said esterification being carried out with the anhydride of the acid containing the group it is desired to enter at the 17- position, or at the 17- and 21- positions, together with a pair of strong acids; and if desired eliminating immediately thereafter any 11-trihaloacetate substituent, to form a compound of formula I, wherein R 2 is hydroxyl, Rs is R 6 , and X, R 1 , R 3 and R 4 are as defined above; or when R 8 is halogen or oxo and R 5 is R 6 , isolating a compound of formula I after the said esterification; or treating a compound of formula IV from the esterification
    wherein R 5 is R 6 , by eliminating the 11-trihaloacetate group therefrom by reaction, in the presence of a lower alcohol, with an organic amine (other than one in which the nitrogen forms part of an aromatic ring), or ammonia gas dissolved in a suitable anhydrous solvent, or ammonium hydroxide or hydrazine, to produce a compound of formula I wherein R 2 is hydroxyl, R 5 is R 6 and X, R 1 , R 3 and R 4 are as defined from formula I; or by so eliminating the 11-trihaloacetate group from a compound of formula
    wherein X, R 1 and R 3 are as defined forformula I; R 9 is an alkyl group of 1 to 3 carbon atoms; and R 10 is a hydrocarbon group comprising one of the following:

    i) an alkyl group of 1 to 16 carbon atoms, whether straight-chained, branched or cyclic;
    ii) an aralkyl group of7 to 8 carbon atoms; or
    iii) a phenyl group;


    to form a compound of formula 1, wherein R 2 and R 5 are both hydroxyls, and R 1 , R 3 , R 4 and X are as defined for formula I.

    Novel steroid derivatives
    8.
    发明公开
    Novel steroid derivatives 失效
    类固醇衍。

    公开(公告)号：EP0393658A2

    公开(公告)日：1990-10-24

    申请号：EP90107415.3

    申请日：1990-04-19

    申请人： SS PHARMACEUTICAL CO., LTD.

    发明人： Komoto, Teruo ,  Okawa, Junji ,  Ogawa, Yoichiro ,  Sato, Susumu ,  Taido, Naokata ,  Kuraishi, Tadayuki

    IPC分类号： C07J5/00 ,  C07J7/00 ,  A61K31/57

    CPC分类号： C07J7/0055 ,  C07J5/0076 ,  C07J7/0085

    摘要： Steroid derivatives represented by formula (I) are disclosed.
    wherein R is a hydrogen atom, a halogen atom, a hydroxy group, or a group -OCOR 1 , wherein R 1 is a linear or branched alkyl group which may be substituted by a halogen atom or a cycloalkyl group, a cycloalkyl group, or an aryl group. The compounds are useful for curing or alleviating inflammation or rheumatism.

    摘要翻译： 公开了由式（I）表示的类固醇衍生物。 其中R为氢原子，卤素原子，羟基或-OCOR1基团，其中R1为可被卤原子或环烷基取代的直链或支链烷基，环烷基， 或芳基。 该化合物可用于治疗或减轻炎症或风湿病。