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    Process for the manufacture of delta 14-20-keto-21-dialkoxy steroids
    11.
    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
    12.
    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。

    Digitoxigenin rhamnoside cyclocarbonates
    18.
    发明授权
    Digitoxigenin rhamnoside cyclocarbonates 失效
    Digitoxigenin鼠李糖苷环状碳酸酯

    公开(公告)号：US3872081A

    公开(公告)日：1975-03-18

    申请号：US37068573

    申请日：1973-06-18

    Applicant: HOECHST AG

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

    IPC: C07J19/00 ,  A61K31/585 ,  A61K31/704 ,  A61P9/04 ,  C07D20060101 ,  C07C173/02

    Abstract: wherein R is hydrogen or alkanoyl or alkyl having 1 to 5 carbon atoms are described as well as two processes for their preparation. The compounds show positive inotropic action and are suitable for treating heart diseases.

    Digitoxigenin-3- Alpha -(L-rhamnopyranoside-2'',3''cyclocarbonates) of the general formula I

    Abstract translation: 对其中R是氢或烷酰基或具有1-5个碳原子的烷基的通式I的二氧化硫脲-3α-[L-鼠李糖吡喃糖苷-2'，3'-环状碳酸酯]以及它们的制备方法进行了描述。 这些化合物显示正性肌力作用，适用于治疗心脏病。

    PROCESS FOR THE MANUFACTURE OF {66 {11 {11 14-20-KETO-21-DIALKOXY STEROIDS
    19.
    发明授权
    PROCESS FOR THE MANUFACTURE OF {66 {11 {11 14-20-KETO-21-DIALKOXY STEROIDS 失效
    制备{66 {11 {11-14-20-酮二十二烷氧基甾体的方法

    公开(公告)号：US3682987A

    公开(公告)日：1972-08-08

    申请号：US3682987D

    申请日：1969-04-14

    Applicant: KURT RADSCHEIT ,  ULRICH STACHE ,  WERNER FRITSCH ,  WERNER HAEDE ,  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, 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.

    Abstract translation: 通过氧化通用制剂的20-KETO-15α，21-二羟基甾体来制备DELTA 14-20-酮二十二烷氧基甾体，其中Y是可被缩合的氧代基团，其可以被醚化或被纯化， DELTA 3-，DELTA 2-或OR DELTA 3,5-ENOL ETHER GROUP或DELTA 3-，DELTA 2-或DELTA 3,5-ENAMINO集团，其组合可能在4位置有双重粘结， 并且是一种较低的ACYCLIC或循环乙酰基化，获得所获得的15α-羟基-20-酮二十一氧代甾族化合物，反应获得的15个α-羟基-20-酮二十二烷氧基异烟肼和治疗 这种15-磺基酸酯可以与分离出酸的试剂一起获得。 这些产品是制造药物的有价值的中间体。

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