c-Met小分子抑制剂XL880的合成

Synthesis of a small molecular inhibitor of c-Met,XL880

目的:合成c-Met小分子抑制剂XL880。方法:以3-甲氧基-4-羟基苯乙酮为起始原料通过7步反应合成了以c-Met为靶的酪氨酸激酶抑制剂XL880(N-{3-氟-4-{6-甲氧基-7-[3-(4-吗啉)丙氧基]喹啉}-4-氧基-苯基}-N-(4-氟苯基)-2,2-二亚甲基丙二酰胺)。结果:目标产物结构经1H-NMR和ESI-MS确证。结论:合成路线短,生产成本低,且合成方法简单温和,方便于小规模制备的实验室研究。

Objective：To synthesize XL880,a small molecular tyrosine inhibitor of c-Met.Methods：U-sing 4-hydroxy-3-methoxy-acetophenone as starting material,XL880,N-{3-fluoro-4-[（6-（methyloxy）-7-{[3-（4-morpholinyl） propyl]oxy}-4-quinolinyl） oxy] phenyl}-N-（4-fluorophenyl）-1,1-cyclopropanedicarboxamide,was synthesized through 7 steps.Results：The structure of XL880 was characterized by 1H-NMR and ESI-MS.Conclusion：This synthesis method is simple and gentle with low cost and short synthetic route,so it is suitable for small-scale preparation in laboratory research.