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    19-alkylene-14- ' -hydroxy-cardenolide derivatives and process for preparing them
    1.
    发明授权
    19-alkylene-14- ' -hydroxy-cardenolide derivatives and process for preparing them 失效
    19-烷基-14-羟基羧酸衍生物及其制备方法

    公开(公告)号：US3859272A

    公开(公告)日：1975-01-07

    申请号：US26961272

    申请日：1972-07-07

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER ,  RADSCHEIT KURT ,  LINDMER ERNAT

    IPC: C07C173/00

    Abstract: Cardiotonically active 19-alkylene-14 Beta -hydroxycardenolides of the formula

    WHEREIN R1 taken alone is -CH, -CO2R5, -CON(R6)2, -CH(OR6)2, C6H5, -CH CH2, or -SCH3, or, taken together with an -OH group in the R3-position, forms a lactone ring; R2 is -H, -CH3, -F, -Cl, Br, or -I; R3 is 5 Alpha -H, 5 Beta -H, or 5 Beta -OH; R4 is -OH, substituted or unsubstituted 3-pyranyl ether, or a 5-or 6membered substituted or unsubstituted cyclic glycoside; R5 is -H, -CH3, -C2H5, -C3H7, -C4H9, -C5H11, or -CH2-C6H5; and R6 is -CH3 or -C2H5, or, when -CH(OR6)2 is a cyclic acetal, the R6''s together are -CH2CH2- or -CH2C(CH3)2CH2-. A process for preparing these compounds from the corresponding 19-oxo-14 Beta hydroxy cardenolides.

    Process for the manufacture of 14beta-hydroxy-3-oxo-5alpha-card-20(22)-enolides
    2.
    发明授权
    Process for the manufacture of 14beta-hydroxy-3-oxo-5alpha-card-20(22)-enolides 失效
    制备14BETA-羟基-3-氧代-5ALPHA-CARD-20（22） - 酚的方法

    公开(公告)号：US3639394A

    公开(公告)日：1972-02-01

    申请号：US3639394D

    申请日：1969-06-25

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER ,  RADSCHEIT KURT

    IPC: C07J19/00 ,  C07C173/00

    CPC classification number: C07J19/00

    Abstract: A 14B-HYDROXY-3-OXO-5A-CARD-20(22)-ENOLIDE IS PREPARED BY KETALIZING A 3-OXO-5A-CARDA-14,20(22)-DIENOLIDE, COVERING THE 3-KETAL SO OBTAINED WITH AN N-HALOGENOAMIDE UNDER WHEAKLY ACID CONDITIONS INTO A 3-KETAL OF A 3-OXO-14B-HYDROXY-15A-BROMO-5A-CARD-20(22)ENOLIDE, CATALYTICALLY HYDROGENATING THIS KETAL TO FORM THE CORRESPONDING 3-OXO-14B-HYDROXY-5A-CARD-20 (22)-ENOLIDE, THE PH VALUE BEING BETWEEN 4.5 AND 7, AND SPLITING OFF THE 3-KETAL GROUP UNDER WEAKLY ACID CONDI TIONS. THE PRODUCTS OF INVENTION HAVE VALUABLE PHARMACOLOGICAL PROPERTIES.

    Process for the manufacture of delta 14-20-keto-21-dialkoxy steroids
    9.
    发明授权
    Process for the manufacture of delta 14-20-keto-21-dialkoxy steroids 失效
    制造DELTA 14-20-酮二十二烷氧基甾体的方法

    公开(公告)号：US3900502A

    公开(公告)日：1975-08-19

    申请号：US15856671

    申请日：1971-06-30

    Applicant: HOECHST AG

    Inventor： RADSCHEIT KURT ,  STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER

    IPC: A61K31/573 ,  A61K31/58 ,  C07C169/32

    CPC classification number: A61K31/573 ,  A61K31/58

    Abstract: Delta 14-20-KETO-21-DIALKOXY STEROIDS ARE PREPARED BY OXIDIZING 20-KETO-15 Alpha ,21-DIHYDROXY STEROIDS OF THE GENERAL FORMULA

    IN WHICH Y is an oxo group which may be ketalized, a

    GROUP WHICH MAY BE ETHERIFIED OR ESTERIFIED, A Delta 3-, Delta 2-, OR Delta 3,5-ENOL ETHER GROUP OR A Delta 3-, Delta 2-, OR Delta 3,5-ENAMINO GROUP, WHICH GROUPS MAY HAVE A DOUBLE BOND IN THE 4-POSITION, AND

    IS A LOWER ACYCLIC OR CYCLIC ACETAL GROUPING, ACETALIZING THE 15 Alpha -HYDROXY-20-KETO-21-OXO STEROIDS OBTAINED, REACTING THE 15 Alpha -HYDROXY-20-KETO-21-DIALKOXY STEROIDS THUS OBTAINED WITH SULFONIC ACID HALIDES AND TREATING THE 15-SULFONIC ACID ESTERS THUS OBTAINED WITH AGENTS SPLITTING OFF ACIDS. The products are valuable intermediates for the manufacture of medicaments.

    Process for manufacture of {62 -(3-oxo-7 {60 -thioa cyl-17{62 -hydroxy-4-androstene-17{60 -yl) propionic acid {65 -lactones
    10.
    发明授权
    Process for manufacture of {62 -(3-oxo-7 {60 -thioa cyl-17{62 -hydroxy-4-androstene-17{60 -yl) propionic acid {65 -lactones 失效
    制备{62-（3-氧代-7 {60-硫代环戊基-17 {62-羟基-4-雄甾烯-17 {6-基）丙酸{65-内酯

    公开(公告)号：US3894006A

    公开(公告)日：1975-07-08

    申请号：US40301873

    申请日：1973-10-03

    Applicant: HOECHST AG

    Inventor： STACHE ULRICH ,  RADSCHEIT KURT

    IPC: C07J31/00 ,  C07D20060101 ,  C07J19/00 ,  C07J21/00 ,  C07C173/00

    CPC classification number: C07J21/00

    Abstract: The present invention relates to an improved process for the manufacture of Beta -(3-oxo-7 Alpha -thioacyl-17 Beta -hydroxy4-androstene-17 Alpha -yl)-propionic acid gamma -lactones in which a Beta -(3-oxo-17 Beta -hydroxy-4,6-androstadiene-17 gamma -yl)-propionaldehyde cyclohemiacetal alkyl glycoside is reacted with a thiocarboxylic acid in a mixture of water and an organic solvent miscible with water to yield a 3-(3''-oxo-7 Alpha ''thioacyl-17 Beta ''-hydroxy-4''-androstene-17 Alpha ''-yl)propionaldehyde cyclohemiacetal alkyl glycoside and in which the compound thus obtained is oxidized in an acid solution, the alkyl glycoside radical in the cyclohemiacetal group being split off, to yield the corresponding gamma -lactone; the invention further relates to new intermediates useful in this process and having the formula

    IN WHICH R1 stands for the methyl group or a hydrogen atom and R2 and R3 each for an alkyl group having 1 to 5 carbon atoms.

    Abstract translation: 本发明涉及制备β-（3-氧代-7α-硫代酰基-17β-羟基-4-雄甾烯-17α-基） - 丙酸γ-内酯的改进方法，其中β-（ 3-氧代-17β-羟基-4,6-雄甾二烯-17γ-基） - 丙醛环氨基乙缩醛烷基糖苷与水与可与水混溶的有机溶剂的混合物中的硫代羧酸反应，得到3-（3 α-氧代-7α-硫代酰基-17β-羟基-4'-雄甾烯-17α-基） - 丙醛环状缩醛烷基糖苷，其中由此获得的化合物在酸性溶液中被氧化，所述烷基糖苷基 在分离出的环状缩甲醛基团中，得到相应的γ-内酯; 本发明还涉及可用于该方法并具有式I的新中间体，其中R 1表示甲基或氢原子，R 2和R 3各自为具有1至5个碳原子的烷基。

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