4-甲基噻唑置于sodium Amide,萘烷体系中,化学反应生成2-氨基-4-甲基噻唑 参考文献:ochiai; Nagasawa,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1938,Vol. 58,P. 1040,1046; Dtsch. Ref. 59 <1939> 43,48 标题:ochiai; Nagasawa,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1938,Vol. 58,P. 1040,1046; Dtsch. Ref. 59 <1939> 43,48
专利信息
专利号:US-8178672-B2 优先权日:2004-10-19 标 题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase 发明人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC 权利人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC; ARQULE INC 摘要:An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.
专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-5215997-A 优先权日:1985-09-11 标题:Synthesis of beta-lactam compounds 发明人:HUNGERBUEHLER ERNST; KALVODA JAROSLAV 权利人:CIBA GEIGY CORP 摘要:The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R 1 is hydrogen or lower alkyl, R 2 is an organic radical which may carry a functional group which may be protected by a customary protective group R 2 o , R 3 is hydrogen or a customary carboxyl protective group R 3 o , W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.
专利号:US-9006421-B2 优先权日:2013-03-14 标题 :Cephalosporin compositions and methods of manufacture 发明人:LAI JAN-JI; PATHARE PRADIP M; KOLLA LAXMA; SORET ADRIEN F 权利人:CUBIST PHARM INC 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
专利号:US-9732097-B2 优先权日:2015-05-11 标 题:Process for the synthesis of a phosphoinositide 3-kinase inhibitor 发明人:ZHOU JIACHENG; QIAO LEI; WENG LINGKAI 权利人:INCYTE CORP 摘要:The present application is directed to processes and intermediates for making (S)-7-(1-((9H-purin-6-yl)amino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, which is an inhibitor of phosphoinositide 3-kinases (PI3Ks), useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 346. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 268. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 291. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 341. 摘要:Shen, Q.; Guo, F.; Hartwig, J. F., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 188.