35853-41-9 = 83012-13-9 反应条件:1.1 Reagents: Phosphorus Oxychloride; 4 H,80 °C 标题:New Hybrid Trifluoromethylquinolines As Antiplasmodium Agents 作者:Da Silva,Renata M. R. J.; Et Al 参考文献:Bioorganic & Medicinal Chemistry 日期:2019 卷标:27(6) 页码:1002-1008]
35853-41-9 = 83012-13-9 反应条件:1.1 Reagents: Phosphorus Oxychloride 标题:A Straightforward And High Yielding Synthesis Of Mefloquine. Ii 作者:Adam,Solange 参考文献:Tetrahedron 日期:1991 卷标:47(36) 页码:7609-14]
372-31-6 = 83012-13-9 反应条件:1.1 3 H,150 °C2.1 Reagents: Phosphorus Oxychloride; 4 H,80 °C 标题:New Hybrid Trifluoromethylquinolines As Antiplasmodium Agents 作者:Da Silva,Renata M. R. J.; Et Al 参考文献:Bioorganic & Medicinal Chemistry 日期:2019 卷标:27(6) 页码:1002-1008]
372-31-6 = 83012-13-9 反应条件:1.1 150 °C2.1 Reagents: Phosphorus Oxychloride; Reflux 标题:Investigations Into The Flexibility Of The 3D Structure And Rigid Backbone Of Quinoline By Fluorine Addition To Enhance Its Blue Emission 作者:Alapour,S.; Et Al 参考文献:Crystengcomm 日期:2018 卷标:20(16) 页码:2316-2323
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:US-2012122923-A1 优先权日:2006-06-13 标 题:Dual molecules containing a peroxide derivative, their synthesis and therapeutic uses 发明人:COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN 权利人:COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN; SANOFI AVENTIS; PALUMED SA; CENTRE NAT RECH SCIENT 摘要:The invention concerns dual molecules corresponding to formula (I): in which: A represents a molecular residue with antimalarial activity of formula (IIa) or (IIIa) or a residue facilitating bioavailability; B represents a cycloalkyl group potentially substituted, or B represents a bi- or tricyclic group capable of being substituted, or B represents 2 cycloalkyl groups linked together through either a single bond or an alkylene chain; m and n represent independently of one another 0, 1 or 2; R 5 represents a hydrogen atom, an alkyl, cycloalkyl or C 1-3 -alkylene-cycloakyl group; Z 1 and Z 2 represent an alkyl radical, the group Z 1 +Z 2 +C i +C j representing a mono- or polycyclic structure, with one of the Z 1 or Z 2 being able to represent a single bond; R 1 and R 2 , identical or different, represent a hydrogen atom or a functional group capable of increasing hydrosolubility; R x and R y forming together a cyclic peroxide including 4 to 8 links and including 1 or 2 additional oxygen atoms in the cyclic structure, possibly substituted by one or more R 3 groups; as a base or a salt to be added to an acid, as a hydrate or solvate, in racemic form, isomers and their mixtures, in addition to their diasteroisomers and their mixtures. Preparation method and use as medications with antimalarial activity.
专利号:HU-P0401607-A2 优先权日:2004-08-10 标题 :Synthesis of aminoquinoline derivatives and of their starting materials
专利号:US-2002188129-A1 优先权日:2001-02-02 标题:One pot synthesis of [2, 8-bis (trifluoromethyl)-4- quinolinyl]2-pyridinylmethanone, a mefloquine intermediate
专利号:RU-2034842-C1 优先权日:1989-07-25 标题:Quinoline derivative and a method of its synthesis
[参考文献]: Sumesh Eswaran, Et Al. New Quinoline Derivatives: Synthesis And Investigation Of Antibacterial And Antituberculosis Properties. Eur J Med Chem. 2010 Aug;45(8):3374-83.
合成参考文献
参考文献:10.1055/s-0031-1290992 摘要:Synthesis of (+)-erythro-Mefloquine Hydrochloride. Synfacts. 2012 May 16;8(06):0594. doi: 10.1055/s-0031-1290992. 参考文献:10.1007/s11030-020-10147-6 摘要:Perković I, Beus M, Schols D, Persoons L, Zorc B. Itaconic acid hybrids as potential anticancer agents. Molecular Diversity. 2020 Oct 11;26(1):1–14. doi: 10.1007/s11030-020-10147-6.