知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

36 条记录 (耗时 0.024 秒)

    Stereospecific total steroidal synthesis via substituted C/D-trans indanones
    2.
    发明授权
    Stereospecific total steroidal synthesis via substituted C/D-trans indanones 失效
    通过取代的C / D反式茚满酮进行立体特异性总体甾体合成

    公开(公告)号：US3984473A

    公开(公告)日：1976-10-05

    申请号：US482711

    申请日：1974-06-24

    申请人： Zoltan George Hajos

    发明人： Zoltan George Hajos

    IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C45/00

    CPC分类号： C07C62/38 ,  C07C62/26 ,  C07C2103/16

    摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1##Wherein m is an integer having a value of 1 or 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonyl and reacting them in the case where R.sub.8 and R.sub.9 taken together are methylene or R.sub.8 is hydrogen and R.sub.9 is methylene-X with .beta.-keto esters and other analogs of the formula ##EQU1## wherein R.sub.6 is selected from the group consisting of ##EQU2## and lower alkyl; R.sub.7 is lower alkyl; R.sub.15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R.sub.25 and R.sub.26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

    摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9是低级烷氧基 - 羰基，芳氧基 - 羰基，低级环烷氧基 - 羰基，羰基 - 卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，并且一起是亚甲基; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基 - 苯甲酰基，三氟乙酰基和樟脑磺酰，并且在R8和R9一起为亚甲基或R8为氢且R9为亚甲基-X与β-酮酯等情况下反应 式O分子R6-CBV的类似物，其中R6选自R26R25 || R7-C-CH-CH2-PAR-CH2R15和低级烷基; R7是低级烷基; R 15选自氧代，低级亚烷基 - 二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。

    Stereospecific total steroidal synthesis via substituted C/D-trans indanones
    3.
    发明授权
    Stereospecific total steroidal synthesis via substituted C/D-trans indanones 失效
    通过取代的C / D反式茚满酮进行立体特异性总体甾体合成

    公开(公告)号：US3910962A

    公开(公告)日：1975-10-07

    申请号：US48282374

    申请日：1974-06-24

    申请人： HOFFMANN LA ROCHE

    发明人： HAJOS ZOLTAN GEORGE

    IPC分类号： C07C62/26 ,  C07C62/38 ,  C07D317/22 ,  C07D317/26 ,  C07D317/30

    CPC分类号： C07C62/38 ,  C07C62/26 ,  C07C2603/16 ,  C07D317/22 ,  C07D317/26 ,  C07D317/30

    摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula

    WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 OR 2; R4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR2) and carbonyl; R8 when taken alone is hydrogen; R9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R8 when taken alone is hydrogen; R9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl; and reacting them in the case where R8 and R9 taken together are methylene or R8 is hydrogen and R9 is methylene-X with Beta -keto esters and other analogs of the formula

    wherein R6 is selected from the group

    consisting of AND LOWER ALKYL; R7 is lower alkyl; R15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R25 and R26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

    摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9为低级烷氧基羰基，芳氧基羰基，低级环烷氧基羰基，羰基卤化物，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团，并且一起为亚甲基时; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基苯甲酰基，三氟乙酰基和樟脑磺酰基; 并且在R 8和R 9一起为亚甲基或R8为氢的情况下使它们反应，并且R 9为亚甲基-X与β-酮酯和式O的其它类似物，其中R6选自R26R25 | | R7 - C - CH --- CH - CH2- PARALLEL R15由和低级ALKYL组成; R7是低级烷基; R 15选自氧代，低级亚烷基二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。

    Oxidative preparation of 3,5-secoandrost-5-one-3,17 .beta.-dioic acid
    8.
    发明授权
    Oxidative preparation of 3,5-secoandrost-5-one-3,17 .beta.-dioic acid 失效
    3,5-二雄甾-5-酮-3,17β-二酸的氧化制备

    公开(公告)号：US5405978A

    公开(公告)日：1995-04-11

    申请号：US158174

    申请日：1993-11-24

    申请人： Paul M. Herrinton

    发明人： Paul M. Herrinton

    IPC分类号： C07C62/24 ,  C07C62/26 ,  C07D303/31 ,  C07J71/00 ,  C07J73/00 ,  C07C61/135

    CPC分类号： C07C62/26 ,  C07C62/24 ,  C07J71/0015 ,  C07J73/005

    摘要： The present invention is an oxidative process for the conversion of 21-unsaturated progesterones (I) ##STR1## to the corresponding 3,5-secoandrost-5-one-3,17.beta.-dioic acids (II) ##STR2## by use of either ozone or an oxidizing agent, which are useful intermediates in the production of .DELTA..sup.5 -4-aza-17-carbonyl steroids (III) which are useful in production of 5.alpha.-4-aza amide (IV) pharmaceuticals. Also disclosed are the novel 21-unsaturated progesterones (I-C) and 3,5-secoandrost-5-one-3,17.beta.-dioic acids (II-C).

    摘要翻译： 本发明是通过使用臭氧或氧化剂转化21-不饱和孕酮（I）罗哌酮-5-一-3,17β-二酸（II）（II）的氧化方法， 它们是生产可用于制备5α-4-氮杂酰胺（IV）药物的DELTA 5-4-氮杂-17-羰基类固醇（III）的有用的中间体。 还公开了新型的21-不饱和孕酮（I-C）和3,5-二雄甾-5-酮-3,17β-二酸（II-C）。

    Process of synthesizing substituted indanones
    9.
    发明授权
    Process of synthesizing substituted indanones 失效
    合成取代茚满酮的方法

    公开(公告)号：US4048195A

    公开(公告)日：1977-09-13

    申请号：US705302

    申请日：1976-07-14

    申请人： Zoltan George Hajos

    发明人： Zoltan George Hajos

    IPC分类号： C07C62/26 ,  C07C62/38 ,  C07D309/12 ,  C07C69/02 ,  C07C69/76 ,  C07C79/46

    CPC分类号： C07C62/26 ,  C07C62/38 ,  C07C2103/16

    摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## WHEREIN M IS AN INTEGER HAVING A VALUE OF 1 TO 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen, R.sub.9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonylAnd reacting them in the case where R.sub.8 and R.sub.9 taken together are methylene or R.sub.8 is hydrogen and R.sub.9 is methylene-X with .alpha.-keto esters and other analogs of the formula ##STR2## wherein R.sub.6 is selected from the group ##STR3## lower alkyl; R.sub.7 is lower alkyl; R.sub.15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonylmethylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R.sub.25 R.sub.26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

    摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物合成类固醇。式IV的双环化合物，其中M是具有1至2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 当单独使用时，R 8为低级烷氧基 - 羰基，芳氧基 - 羰基，低级环烷基氧基 - 羰基，羰基 - 卤素，氢，羧基，甲酰基和亚甲基-X，其中X为离去基团 是亚甲基; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基苯甲酰基，三氟乙酰基和樟脑磺酰，并在其中反应。其中R8和R9一起为亚甲基或R8为氢，R9为亚甲基-X与α-酮酯和其他类似物 式VI其中R 6选自低级烷基; R7是低级烷基; R 15选自氧代，低级亚烷基 - 二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25 R 26独立地选自氢，羟基和 低级烷基。

    Stereospecific total steroidal synthesis via substituted C/D-trans indanones
    10.
    发明授权
    Stereospecific total steroidal synthesis via substituted C/D-trans indanones 失效
    通过取代的C / D反式茚满酮进行立体特异性总体甾体合成

    公开(公告)号：US3985733A

    公开(公告)日：1976-10-12

    申请号：US482709

    申请日：1974-06-24

    申请人： Zoltan George Hajos

    发明人： Zoltan George Hajos

    IPC分类号： C07C62/26 ,  C07C62/38 ,  C07C119/00

    CPC分类号： C07C62/26 ,  C07C62/38 ,  C07C2103/16

    摘要： Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1##Wherein m is an integer having a value of 1 or 2; R.sub.4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR.sub.2) and carbonyl; R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is lower alkoxy-carbonyl, aryloxy-carbonyl, lower cycloalkyloxy-carbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R.sub.8 when taken alone is hydrogen; R.sub.9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R.sub.2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxy-benzoyl, trifluoroacetyl and camphorsulfonylAnd reacting them in the case where R.sub.8 and R.sub.9 taken together are methylene or R.sub.8 is hydrogen and R.sub.9 is methylene-X with .beta.-keto esters and other analogs of the formula ##EQU1## wherein R.sub.6 is selected from the group CONSISTING OF ##EQU2## and LOWER ALKYL; R.sub.7 is lower alkyl; R.sub.15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R.sub.25 and R.sub.26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.

    摘要翻译： 已知的促孕活性甾体材料的全合成。 可以根据通过使用作为中间体选择的特定起始反应物来合成类固醇，其具有下式的双环化合物，其中M是具有1或2的值的整数; R4是氢或低级烷基; Z是低亚烷基二氧基，CH（OR 2）和羰基; 单独使用时为R8; 当单独使用时，R 9是低级烷氧基 - 羰基，芳氧基 - 羰基，低级环烷氧基 - 羰基，羰基 - 卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，并且一起是亚甲基; 条件是当Z为羰基时，当单独使用时为氢; 当单独使用时，R 9是卤素，氢，羧基，甲酰基和亚甲基-X，其中X是离去基团，当它们一起是亚甲基且R 2是氢时，低级烷基，低级烷氧基 - 低级烷基，苯基 - 低级烷基，四氢吡喃基， 低级烷酰基，苯甲酰基，硝基苯甲酰基，羧基 - 低级烷酰基，羧基 - 苯甲酰基，三氟乙酰基和樟脑磺酰，并反应其中R 8和R 9一起为亚甲基或R8为氢，R9为亚甲基-X，带有β-酮酯等 式O分子R6-CBV的类似物，其中R 6选自R 26 R 25 | R 7 -C-CH-CH 2 - 并行R 15和低级烷基; R7是低级烷基; R 15选自氧代，低级亚烷基二氧基或（氢和低级烷氧基）; B选自低级烷氧基 - 羰基 - 亚甲基，低级 - 芳氧基 - 羰基 - 亚甲基，氰基亚甲基，低级烷基亚磺酰基 - 亚甲基，低级烷基磺酰基 - 亚甲基，R 25和R 26独立地选自氢 ，羟基和低级烷基。