专利号:US-2010184989-A1 优先权日:2007-03-12 标 题 :De Novo Synthesis of Conjugates 发明人:RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J 权利人:NEKTAR THERAPEUTICS 摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.
专利号:AU-2008226820-A1 优先权日:2007-03-12 标题 :De novo synthesis of conjugates
专利号:CA-2679473-A1 优先权日:2007-03-12 标题:De novo synthesis of conjugates
专利号:US-4072716-A 优先权日:1971-12-24 标 题:Bicycloalkane derivatives 发明人:SAUER GERHARD; HAUSER HELMUT; HAFFER GREGOR; RUPPERT JUERGEN; EDER ULRICH; WIECHERT RUDOLF 权利人:SCHERING AG 摘要:Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R 1 is lower alkyl, X is carbonyl or free or etherified hydroxymethylene, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is alkyl, R 3 is hydrogen or lower alkyl, R 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 2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.
专利号:US-4051188-A 优先权日:1971-12-24 标题 :Novel bicycloalkane derivatives and the production thereof 发明人:SAUER GERHARD; HAUSER HELMUT; HAFFER GREGOR; RUPPERT JUERGEN; EDER ULRICH; WIECHERT RUDOLF 权利人:SCHERING AG 摘要:Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R 1 is lower alkyl, X is carbonyl or a free or etherified hydroxymethylene, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is aryl or aralkyl, R 3 is hydrogen or lower alkyl, R 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 2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.
专利号:US-4008253-A 优先权日:1971-12-24 标题 :Bicycloalkanes 发明人:SAUER GERHARD; HAUSER HELMUT; HAFFER GREGOR; RUPPERT JURGEN; EDER ULRICH; WIECHERT RUDOLF 权利人:SCHERING AG 摘要:Bicycloalkane derivatives of the formula ##STR1## WHEREIN N IS 1 OR 2, R 1 is lower alkyl, X is free or ketalized carbonyl or a free, esterified, or etherified hydroxymethylene, and Y is --S--R 2 , --SO m --R 2 , or ##STR2## wherein m is 1 or 2, R 2 is alkyl, aryl, or aralkyl, R 3 is hydrogen or lower alkyl, R 4 is alkoxycarbonyl, or acyl or phenyl optionally substituted with lower alkoxy or benzyloxy- or acyloxy; and Z is nitrile, 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 2 Y substituent with formaldehyde and a mercaptan or a sulfinic acid, followed if desired by oxidation and optional salt condensation.
[参考文献]: T Kametani, Et Al. Antispasmodic Agents. 1. Syntheses And Pharmacological Activity Of Aminoalkyl 3-Substituted Phenylacetates. J Med Chem. 1971 Jan;14(1):72-5.
合成参考文献
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 70. 摘要:Marsden, S. P., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 607. 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 355. 摘要:Ying, J.; Wu, X.-F., Science of Synthesis: Knowledge Updates, (2024) 1, 291.