Nanterinone, UK-61260-27(mesylate), UK-61260
6-(2,4-二甲基咪唑-1-基)-8-甲基-1H-喹啉-2-酮 6-(2,4-二甲基咪唑-1-基)-8-甲基-1h-喹啉-2-酮甲烷磺酸 Chemical Name: 6-(2,4-Dimethylimidazol-1-yl)-8-methylquinolin-2(1H)-one
CAS No. 102791-47-9, 102791-74-2 (mesylate salt)
项目整合开发状态: Phase II
项目研究机构: Pfizer (Originator)
合成路线:The condensation of 4-fluoro-2-methylnitrobenzene (I) with 2,4-dimethyl-1H-imidazole (II) by means of Na2CO3 in hot DMF gives 4-(2,4-dimethyl-1H-imidazol-1-yl)-2-methylnitrobenzene (III),which is reduced with SnCl2 in refluxing ethanol yielding the corresponding aniline (IV).The condensation of (IV) with trans-3-ethoxypropenoyl chloride in anhydrous pyridine affords the anilide (VI),which is finally cyclized by means of 98% H2SO4.
📌 参考资料/链接：
参考文献标题:Quinolone inotropic agents
文献作者:Roberts,D.A.; Campbell,S.F.(Pfizer Inc.)
参考来源:AU 8543032; EP 0166533; ES 8608874; ES 8801797; JP 1986000082; US 4728653
📄 详细内容
合成路线:The condensation of 4-fluoro-2-methylnitrobenzene (I) with 2,4-dimethyl-1H-imidazole (II) by means of Na2CO3 in hot DMF gives 4-(2,4-dimethyl-1H-imidazol-1-yl)-2-methylnitrobenzene (III),which is reduced with SnCl2 in refluxing ethanol yielding the corresponding aniline (IV).The condensation of (IV) with trans-3-ethoxypropenoyl chloride in anhydrous pyridine affords the anilide (VI),which is finally cyclized by means of 98% H2SO4.
参考文献标题:NANTERINONE < Prop INN>
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1989,14(4),328
合成路线:The condensation of 4-fluoro-2-methylnitrobenzene (I) with 2,4-dimethyl-1H-imidazole (II) by means of Na2CO3 in hot DMF gives 4-(2,4-dimethyl-1H-imidazol-1-yl)-2-methylnitrobenzene (III),which is reduced with SnCl2 in refluxing ethanol yielding the corresponding aniline (IV).The condensation of (IV) with trans-3-ethoxypropenoyl chloride in anhydrous pyridine affords the anilide (VI),which is finally cyclized by means of 98% H2SO4.
参考文献标题:2(1H)-Quinolinones with cardiac stimulant activity.2.Synthesis and biological activities of 6-(N-linked,five-membered heteroaryl) derivatives
文献作者:Alabaster,C.T.; Bell,A.S.; Campbell,S.F.; Ellis,P.; Henderson,C.G.; Morris,D.S.; Roberts,D.A.; Ruddock,K.S.; Samuels,G.M.R.; Stefaniak,M.H.
参考来源:J Med Chem 1989,32(3),575-83
产品链接: CAS No. 102791-47-9›› 产品链接: CAS No.102791-74-2››