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新产品编号:1571435

Chemical Name: 3-[2-Amino-3-(pivaloyl)imidazo[1,2-a]pyridin-6-yl]-N-methyl-3-phenyl-2(E)-propenamide
项目整合开发状态: Biological Testing
项目研究机构: Lilly (Originator)
合成路线:Ketone (III) was prepared by Friedel-Crafts acylation of benzene (II) with 6-chloronicotinyl chloride (I).Horner-Emmons reaction of (III) with diethyl (N-methylcarbamoylmethyl)phosphonate (IV) using potassium hexamethyl-disilazide produced a 3:1 mixture of E (V) and Z olefins (VI).The desired E isomer (V) was isolated by column chromatography and then treated with bromoketone (VII) to afford the betaine (VIII).Finally,the target imidazopyridine was obtained by condensation of (VIII) with cyanamide in the presence of K2CO3.
📌 参考资料/链接:
参考文献标题:Short synthesis and anti-rhinoviral activity of imidazo[1,2-a]pyridines: The effect of acyl groups at 3-position
文献作者:Hamdouchi,C.; Ezquerra,J.; Vega,J.A.; Vaquero,J.J.; Alvarez-Builla,J.; Heinz,B.A.
参考来源:Bioorg Med Chem Lett 1999,9(10),1391