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新产品编号:1278765

Chemical Name: (Z)-4-(4-Phenyl-1-butenyl)-1H-imidazole fumarate
项目整合开发状态: Preclinical
项目研究机构: Bioprojet (Originator)
合成路线:The Wittig condensation of 1-tritylimidazole-4-carbaldehyde (I) with triphenyl(3-phenylpropyl)phosphonium bromide (II) and potassium tert-butoxide in THF gives 4-(4-phenyl-1(Z)-butenyl)-1-trityl-1H-imidazole (III),which is deprotected with 6N HCl in refluxing acetone.

合成路线:The Wittig condensation of 1-tritylimidazole-4-carbaldehyde (I) with triphenyl(3-phenylpropyl)phosphonium bromide (II) and potassium tert-butoxide in THF gives 4-(4-phenyl-1(Z)-butenyl)-1-trityl-1H-imidazole (III),which is deprotected with 6N HCl in refluxing acetone yielding 4-(4-phenyl-1(Z)-butenyl)-1H-imidazole (IV).Finally,this compound is hydrogenated with H2 over Pd/C in methanol.
📌 参考资料/链接:
参考文献标题:General construction pattern of histamine H3-receptor antagonists: Change of a paradigm
文献作者:Stark,H.; Ligneau,X.; Arrang,J.-M.; Schwartz,J.-C.; Schunack,W.
参考来源:Bioorg Med Chem Lett 1998,8(15),2011