Tariquidar, XR-9576
2-醛基-4-甲氧基苯硼酸Chemical Name: N-[2-[N-[4-[2-(6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide
CAS No. 206873-63-4
项目整合开发状态: Phase II
项目研究机构: Xenova (Originator), QLT PhotoTherapeutics (Licensee), National Cancer Institute (Codevelopment)
合成路线:4,5-Dimethoxy-2-nitrobenzoic acid (I) was converted to the corresponding acid chloride (II) upon treatment with SOCl2,and this was further coupled to aniline (III),producing amide (IV).Catalytic hydrogenation of the nitro group of (IV) afforded amine (V).Acid chloride (VII) --obtained by chlorination of 3-quinolinecarboxylic acid (VI) with SOCl2-- was then condensed with amine (V) to furnish the title diamide.
📌 参考资料/链接：
参考文献标题:Anthranilic acid derivs.as multi drug resistance modulators
文献作者:Ryder,H.; Ashworth,P.A.; Roe,M.J.; Brumwell,J.E.; Hunjan,S.; Folkes,A.J.; Sanderson,J.T.; Williams,S.; Maximen,L.M.(Xenova Group plc)
参考来源:EP 0934276; GB 2334521; JP 2001502683; US 6218393; WO 9817648
📄 详细内容
合成路线:4,5-Dimethoxy-2-nitrobenzoic acid (I) was converted to the corresponding acid chloride (II) upon treatment with SOCl2,and this was further coupled to aniline (III),producing amide (IV).Catalytic hydrogenation of the nitro group of (IV) afforded amine (V).Acid chloride (VII) --obtained by chlorination of 3-quinolinecarboxylic acid (VI) with SOCl2-- was then condensed with amine (V) to furnish the title diamide.
参考文献标题:Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives
文献作者:Roe,M.; Folkes,A.; Ashworth,P.; Brumwell,J.; Chima,L.; Hunjan,S.; Pretswell,I.; Dangerfield,W.; Ryder,H.; Charlton,P.
参考来源:Bioorg Med Chem Lett 1999,9(4),595
产品链接: CAS No. 206873-63-4››