4-氯喹啉-N-氧化物置于zinc Trifluoromethanesulfonate体系中,用 乙腈 作为反应溶剂,化学反应 1.08H,以79%的收率获得产物4-氯喹啉 参考文献:An Efficient And General Method For The Deoxygenation Of Organic N-Oxides Using Zn(Otf)2 And Cu(Otf)2 标题:An Efficient And General Method For The Deoxygenation Of Organic N-Oxides Using Zn(Otf)2 And Cu(Otf)2 摘要:本文描述了一种温和且高效的通用方法,利用zn(Otf)2和cu(Otf)2对有机n-氧化物(如偶氮苯,N-芳基亚硝胺和n-杂环n-氧化物)进行脱氧反应,产率优异. DOI:10.1055/s-2006-926269
专利号:US-6472534-B2 优先权日:1999-10-21 标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors 发明人:BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K 权利人:AGOURON PHARMA 摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
专利号:US-6500955-B1 优先权日:2001-02-02 标 题:One pot synthesis of [2,8-Bis (trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, a mefloquine intermediate 发明人:CHAWLA HARMANDER PAL SINGH; JOHAR PERMINDER SINGH; MITTAL ALKA; MEENA RAM AVTAR; NEGI VILLENDRA SINGH 权利人:NAT INST OF PHARMACEUTICAL EDU 摘要:The present invention provides a simple single step process for the preparation of [2,8-bis(trifluoromethyl)-4-quinolinyl]-2-pyridinylmethanone, comprising the step of condensing a halo-quinoline with an alpha-picolyl derivatives in the presence of a solvent, a base and a phase transfer catalyst at −10° C. to +90° C.
专利号:WO-2010144434-A1 优先权日:2009-06-09 标题 :Derivatives of mefloquine and associated methods for making and using 发明人:DOW GEOFFREY S; MILNER ERIN E; WIPF PETER; MO TINGTING 权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF THE ARMY ON BEHALF OF U S; DOW GEOFFREY S; MILNER ERIN E; WIPF PETER; MO TINGTING 摘要:The present invention relates to new mefloquine derivatives and therapeutic compositions comprising one or more mefloquine derivatives. Mefloquine derivatives of the invention have a pentafluorosulfanyl moiety substitution at the 8-position. Certain mefloquine derivatives further include a quinoline methanol moiety substitution at the 4-position. The present invention also relates to new intermediate compounds useful in the synthesis of the mefloquine derivatives, which intermediates also have a pentafluorosulfanyl moiety substitution at the 8-position.
专利号:US-3989691-A 优先权日:1973-01-05 标 题 :Preparation of cinchona alkaloid intermediates 发明人:TAYLOR EDWARD C; MARTIN STEPHEN F 权利人:UNIV PRINCETON 摘要:4-[3-(3-vinyl-1-acetyl-4-piperidyl)-1-propenyl]-6-methoxyquinoline, the corresponding epoxide and related compounds, useful in the synthesis of Cinchona alkaloids, are prepared by introducing an ylid group in the 4-position of a suitably substituted quinoline and reacting this ylid with an N-acetyl-4-piperidineacetaldehyde.
专利号:US-2002038033-A1 优先权日:1999-10-21 标题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
专利号:US-2003023092-A1 优先权日:1999-10-21 标题 :Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors
[参考文献]: Tamara Rodríguez-Cabo, Et Al. Time-Of-Flight Accurate Mass Spectrometry Identification Of Quinoline Alkaloids In Honey. Anal Bioanal Chem. 2015 Aug;407(20):6159-70.
合成参考文献
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 417. 摘要:Braverman, S.; Cherkinsky, M., Science of Synthesis Knowledge Updates, (2014) 3, 292. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 22. 摘要:Denmark, S.; Chang, W.-T. T., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 407. 摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 654.