CAS: 53230-10-7; (S)-(2,8-Bis(Trifluoromethyl)Quinolin-4-yl)((R)-Piperidin-2-yl)Methanol

该化合物是一种主要用作抗疟剂的合成quinoline衍生物,对抗氯quine的恶性疟原虫菌株有效,在流行病地区的预防和治疗疟疾疗程中具有价值. 蛋白质通过干扰寄生虫的消化真空,导致细胞中毒性肝炎累积,其长的半衰期(~21天)允许每周服用剂量,改善病人在预防用途方面的合规性. 化合物表现出高生物利用率和广泛的组织分布,包括渗透到红细胞中. 然而,...

结构式图片

MSDS等安全信息

    上下游产品

    tert-butyl (S)-2-((R)-(2,8-bis(trifluoromethyl)quinolin-4-yl)(hydroxy)methyl)-5,6-dihydropyridine-1(2H)-carboxylate (S)-tert-butyl 2-((R)-(2,8-bis(trifluoromethyl)quinolin-4-yl)(hydroxy)methyl)piperidine-1-carboxylate (+)-(11S,12R)-erythro-mefloquine, O,O-(-)-di-p-toluoyl-L-tartrate 2,8-bis(trifluoromethyl)quinolin-4-ol(2,8-bis-trifluoromethyl-quinolin-4-yl)-piperidin-2-yl-methanol; hydr°Chloride (R)-2-((S)-(2,8-bis(trifluoromethyl)quinolin-4-yl)(hydroxy)methyl)piperidin-1-ium chloride (R)-tert-butyl 2-((S)-(2,8-bis(trifluoromethyl)quinolin-4-yl)(hydroxy)methyl)piperidine-1-carboxylate (+)-(11S,12R)-erythro-mefloquine-(R)-mosher amide

    合成工艺路线路线简述

      海关参考信息

      专利信息


      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-2024287041-A1
      优先权日:2021-05-20
      标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms
      发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN
      权利人:KARYOPHARM THERAPEUTICS INC
      摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.

      专利号:WO-2012107532-A1
      优先权日:2011-02-11
      标 题 :4-aminoalcoholquinoline derivatives, enantioselective synthesis methods and the use thereof
      发明人:JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL
      权利人:UNIV PICARDIE; JONET ALEXIA; DASSONVILLE-KLIMPT ALEXANDRA; MULLIE CATHERINE; TAUDON NICOLAS; SONNET PASCAL
      摘要:The present invention is intended to provide new antimalarial compounds with a strong antimalarial activity as well as antibacterial activity with few neurological side effects and a new enantioselective pathway to mefloquine amino-analogs allowing the access of such compounds. The present invention relates to new 4 -aminoalcohol quinoline derivatives of formula (I), as well as the synthesis methods and the uses of such derivatives. In which Y is one selected from formulae (II) to (III). In which Z is selected from formulae (IV) to (VI), and wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and n are as defined in the claims.

      专利号:US-9994558-B2
      优先权日:2013-09-20
      标题 :Multicyclic compounds and methods of using same
      发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
      权利人:KARYOPHARM THERAPEUTICS INC
      摘要:The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).

      专利号:WO-2022246227-A1
      优先权日:2021-05-20
      标 题:Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms

      专利号:US-10363247-B2
      优先权日:2015-08-18
      标 题:(S,E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(3-fluoro-3-methylpyrrolidine-1-carbonyl)phenyl-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide for the treatment of cancer
      发明人:BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM
      权利人:KARYOPHARM THERAPEUTICS INC
      摘要:The invention generally relates to substituted benzofuranyl compounds and, more particularly, to a compound represented by Structural Formula 1a: (I) or a pharmaceutically acceptable salt thereof. The invention also includes the synthesis and use of the compound of Structural Formula 1a, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of diseases or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disease) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.

      供应商参考报价(招募中)

      品牌试剂参考报价(招募中)

      📌 第三方产品分析报告

      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Keiser J, Silué KD, Adiossan LK, N'Guessan NA, Monsan N, Utzinger J, N'Goran EK. Praziquantel, mefloquine-praziquantel, and mefloquine-artesunate-praziquantel against Schistosoma haematobium: a randomized, exploratory, open-label trial. PLoS Negl Trop Dis. 2014 Jul 17;8(7):e2975. doi: 10.1371/journal.pntd.0002975. eCollection 2014 Jul.
      2: Janowsky A, Eshleman AJ, Johnson RA, Wolfrum KM, Hinrichs DJ, Yang J, Zabriskie TM, Smilkstein MJ, Riscoe MK. Mefloquine and psychotomimetics share neurotransmitter receptor and transporter interactions in vitro. Psychopharmacology (Berl). 2014 Jul;231(14):2771-83. doi: 10.1007/s00213-014-3446-0. Epub 2014 Feb 2.
      3: Tao Y, Xue J, Jiang B, Zhang HB, Xiao SH. Significance of higher drug concentration in erythrocytes of mice infected with Schistosoma japonicum and treated orally with mefloquine at single doses. Parasitol Res. 2015 Dec;114(12):4521-30. doi: 10.1007/s00436-015-4696-4. Epub 2015 Sep 4. doi: 10.1186/s13104-015-1088-x.

      合成参考文献


      参考文献:10.1016/j.bmcl.2015.09.034
      摘要:Russo CM, Adhikari AA, Wallach DR, Fernandes S, Balch AN, Kerr WG, Chisholm JD. Synthesis and initial evaluation of quinoline-based inhibitors of the SH2-containing inositol 5′-phosphatase (SHIP). Bioorganic & Medicinal Chemistry Letters. 2015 Nov;25(22):5344–8. doi: 10.1016/j.bmcl.2015.09.034.
      📝 需求与反馈
      尽可能描述清楚需求与问题信息
      ×

      通知