公开(公告)号：US4202991A

公开(公告)日：1980-05-13

申请号：US753996

申请日：1976-12-27

申请人： Gerhard Sauer ,  Helmut Hauser ,  Gregor Haffer ,  Juergen Ruppert ,  Ulrich Eder ,  Rudolf Wiechert

发明人： Gerhard Sauer ,  Helmut Hauser ,  Gregor Haffer ,  Juergen Ruppert ,  Ulrich Eder ,  Rudolf Wiechert

IPC分类号： C07C317/00 ,  C07D317/30 ,  C07D317/46 ,  C07D319/06 ,  C07C69/145 ,  C07C69/24

CPC分类号： C07D319/06 ,  C07C317/00 ,  C07C321/00 ,  C07D317/30 ,  C07D317/46

摘要： Bicycloalkane derivatives of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is lower alkyl, Acyl is alkanoyl, and Y is --S--R.sub.2, --SO.sub.m --R.sub.2, or ##STR2## wherein m is 1 or 2, R.sub.2 is alkyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is acyl or phenyl optionally substituted with lower alkoxy, benzyloxy or alkanoyloxy; and Z is nitro, lower alkoxycarbonyl, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH.sub.2 Y substituent with formaldehyde and a mercaptan or sulfinic acid, followed if desired by oxidation and optional salt condensation.

摘要翻译： 其中n为1或2，R 1为低级烷基，酰基为烷酰基，Y为-S-R 2，-SO m -R 2或者其中m为1或2，R 2为 烷基，R 3是氢或低级烷基，R 4是任选被低级烷氧基，苄氧基或烷酰氧基取代的酰基或苯基; Z是硝基，低级烷氧基羰基，低级烷酰基，低级烷基亚磺酰基或低级烷基磺酰基是类固醇总合成中的有用中间体。 通过使缺少CH 2 Y取代基的相应化合物与甲醛和硫醇或亚磺酸反应制备化合物，随后如果需要，通过氧化和任选的盐缩合。

公开(公告)号：US4051188A

公开(公告)日：1977-09-27

申请号：US753997

申请日：1976-12-27

申请人： Gerhard Sauer ,  Helmut Hauser ,  Gregor Haffer ,  Juergen Ruppert ,  Ulrich Eder ,  Rudolf Wiechert

发明人： Gerhard Sauer ,  Helmut Hauser ,  Gregor Haffer ,  Juergen Ruppert ,  Ulrich Eder ,  Rudolf Wiechert

IPC分类号： C07D317/30 ,  C07D317/46 ,  C07C49/76

CPC分类号： C07D317/30 ,  C07D317/46

摘要： Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R.sub.1 is lower alkyl, X is carbonyl or a free or etherified hydroxymethylene, and Y is --S--R.sub.2, --SO.sub.m --R.sub.2, or ##STR2## wherein m is 1 or 2, R.sub.2 is aryl or aralkyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is phenyl optionally substituted with lower alkoxy or benzyloxy, and Z is nitro, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl, are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH.sub.2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.

公开(公告)号：US4072716A

公开(公告)日：1978-02-07

申请号：US754000

申请日：1976-12-27

申请人： Gerhard Sauer ,  Helmut Hauser ,  Gregor Haffer ,  Juergen Ruppert ,  Ulrich Eder ,  Rudolf Wiechert

发明人： Gerhard Sauer ,  Helmut Hauser ,  Gregor Haffer ,  Juergen Ruppert ,  Ulrich Eder ,  Rudolf Wiechert

IPC分类号： C07D317/30 ,  C07D317/46 ,  C07C49/54

CPC分类号： C07D317/46 ,  C07D317/30

摘要： Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R.sub.1 is lower alkyl, X is carbonyl or free or etherified hydroxymethylene, and Y is --S--R.sub.2, --SO.sub.m --R.sub.2, or ##STR2## wherein m is 1 or 2, R.sub.2 is alkyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is aliphatic acyl and Z is nitro, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH.sub.2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.

摘要翻译： 式中，R 1为低级烷基，X为羰基或游离的或醚化的羟基亚甲基，Y为-S-R 2，-SO m-R 2或其中m为1的双环烷烃衍生物 或2，R2是烷基，R3是氢或低级烷基，R4是脂族酰基，Z是硝基，低级烷酰基，低级烷基亚磺酰基或低级烷基磺酰基是在类固醇的总合成中的有用的中间体。 通过使相应的缺少CH 2 Y取代基的化合物与甲醛和硫醇或亚磺酸反应来制备化合物，随后如果需要，通过氧化和任选的盐缩合。