专利号:US-2006264608-A1 优先权日:2001-08-03 标题 :Bi-directional synthesis of oligoguanidine transport agents 发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
专利号:US-7067698-B2 优先权日:2001-08-03 标 题 :Bi-directional synthesis of oligoguanidine transport agents 发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
专利号:US-6951932-B2 优先权日:2001-10-25 标 题:Synthesis of 2-aralkoxyadenosines and 2-alkoxyadenosines 发明人:MOORMAN ALLAN R 权利人:KING PHARMACEUTICALS RES & DEV 摘要:The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine. Preferred methods of the invention include activating a guanosine compound followed by hydrolysis; alkylating the hydrolyzed compound with subsequent animation to provide a 2-aralkyloxyadenosine or a 2-alkoxyadenosine compound.
专利号:US-5554725-A 优先权日:1994-09-14 标题:Synthesis of dolastatin 15 发明人:PETTIT GEORGE R 权利人:UNIV ARIZONA 摘要:The present invention relates to the synthesis of natural (-)- dolastatin and the elucidation of the absolute configuration of this important sea hare constituent. A segment synthetic strategy was utilized for obtaining the Dolabella auricularia (Indian Ocean sea hare) depsipeptide dolastatin 15. Reaction of protected (S)-Hiva-(S)-Phe (2c) with isopropenyl chloroformate followed by Meldrum's ester, cyclization (2c→3a) of the product in toluene and finally methylation afforded the key (S)-dolapyrrolidine (Dpy) derivative (3b). Condensation of tripeptide (8) with the three unit Dpy segment (5b) followed by deprotection and coupling (diethyl phosphorocyanidate) led to dolastatin 15 in 11% overall yield. The powerful and selective activity of dolastatin 15 against the U.S. National Cancer Institute's panel of human cell lines is reported.
专利号:US-5656662-A 优先权日:1990-01-12 标 题:Synthesis of optically pure 4-alkenyl- or 4-alkanyl-2-hydroxytetronic acids 发明人:MANTRI PADMAJA; WITIAK DONALD T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, thus making them useful in the treatment of coronary artery diseases, especially atherosclerosis, and additionally, as inhibitors of various inflammatory cytokines, making them useful in the treatment of both acute and chronic inflammation, as well in the treatment of cachexia, rheumatoid arthritis, multiple sclerosis, Crohn's disease and ulcerative colitis. The invention further relates to pharmaceutical compositions of the instant compounds.
专利号:EP-1575929-B1 优先权日:2002-12-19 标 题 :The method for production of semi-finished products useful in synthesis of paclitaxel 发明人:KOLESINSKA BEATA; KAMINSKI J ZBIGNIEW; KAMINSKA E JANINA 权利人:AGROPHARM S A 摘要:The method for production of the semi-finished products useful in synthesis of Paclitaxel with the generalized formula (2), characterized in that phenyl isoserine derivatives, or mixtures of their epimerides with various configurations on the carbon 2' or their salts, are treated with triazine type condensing agent, possible in the presence of tertiary amine, in medium of anhydrous organic solvent, and the triazine esters produced are treated with Baccatin III, in medium of anhydrous organic solvent, possible in the presence of a catalyst.
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合成参考文献
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