专利号:US-2004249170-A1 优先权日:2002-01-24 标 题 :Process for preparing an intermediate useful for the asymmetric synthesis of duloxetine 发明人:BORGHESE ALFIO 摘要:This invention provides a process for the synthesis of(S)-3-Methylamino-1-2-thienyl)-1-propanol, a key intermediate in the synthesis of duloxetine.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-2007015798-A1 优先权日:2005-02-25 标 题 :Efficient and stereoselective process for large scale synthesis of (3R)-3-(2,3-dihydrobenzofuran-5-yl)-1,2,3,4-tetrahydropyrrolo[3,4-b]quinolin-9-one derivatives 发明人:LI XUN; LEMAIRE SEBASTIEN; MARKO ISTVAN; WILLEMSENS ALBERT 权利人:LI XUN; LEMAIRE SEBASTIEN; MARKO ISTVAN; WILLEMSENS ALBERT 摘要:This invention relates to an efficient process for large scale stereoselective production of (3R)-3-(2,3-dihydrobenzofuran-5-yl)-1,2,3,4-tetrahydropyrrolo[3,4-b]quinolin-9-ones and key intermediates used for the preparation of benzofuranyl pyrroloquinolones as potent and selective PDE5 inhibitors for the treatment of erectile dysfunction, as well as pharmaceutical compositions and methods of treatment utilizing these compounds.
专利号:US-11981648-B2 优先权日:2019-06-13 标题:Method for the synthesis of 3-R-1,4,2-dioxazol-5-ones 发明人:HALL DAVID S; DAHN JEFFERY RAYMOND; HYNES TOREN 权利人:TESLA INC; PANASONIC HOLDINGS CORP 摘要:Provided are methods of preparing 3-R-1,4,2-dioxazol-5-one compounds using convenient and efficient methods. Also provided are 3-R-1,4,2-dioxazol-5-one compounds produced using the methods described.
专利号:US-4835280-A 优先权日:1985-01-18 标 题 :Indoline compounds for synthesis of pharmaceutically active pyrrolobenzimidazoles 发明人:MARTENS ALFRED; HOELCK JENS-PETER; BERGER HERBERT; MUELLER-BECKMAN BERND; STREIN KLAUS; ROESCH EGON 权利人:BOEHRINGER MANNHEIM GMBH 摘要:The present invention provides Indolines of the formula: (II) (III) ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: (I) These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.
专利号:US-7034154-B2 优先权日:1999-08-10 标 题:Synthesis of substituted pyrazolopyrimidines 发明人:GROSS RAYMOND S; WILCOXEN KEITH M; OGLESBY RICHARD CHRISTOPHER 权利人:NEUROCRINE BIOSCIENCES INC 摘要:Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
摘要:Snaith, J. S., Science of Synthesis Knowledge Updates, (2011) 2, 234. 摘要:Okamoto, K.; Ohe, K., Science of Synthesis Knowledge Updates, (2020) 1, 148. 摘要:Lubell, W. D.; St-Cyr, D. J.; Dufour-Gallant, J.; Hopewell, R.; Boutard, N.; Kassem, T.; Dörr, A.; Zelli, R., Science of Synthesis Knowledge Updates, (2013) 1, 177. 摘要:Stanforth, S. P., Science of Synthesis Knowledge Updates, (2014) 3, 31. 摘要:Davies, G. H. M.; Wisniewski, S. R., Science of Synthesis Knowledge Updates, (2021) 2, 214.