ICA-17043
4-氟-A-(4-氟苯基)-A-苯基-苯甲酰胺Chemical Name: 2,2-Bis(4-fluorophenyl)-2-phenylacetamide
CAS No. 289656-45-7
项目整合开发状态: Phase II
项目研究机构: ICAgen (Orphan Drug), ICAgen (Originator), McNeil Consumer Products (Codevelopment)
合成路线:The Grignard condensation of 4,4'-difluorobenzophenone (I) with phenylmagnesium bromide (II) in refluxing tert-butyl methyl ether gives the corresponding carbinol (III),which is treated with acetyl chloride in dichloromethane to yield the methyl chloride (IV).Condensation of compound (IV) with copper cyanide by heating at 140 癈,followed by treatment with hot toluene affords 2,2-bis(4-fluorophenyl)-2-phenylacetonitrile (V),which is finally partially hydrolyzed with H2SO4 in refluxing glacial acetic acid.
📌 参考资料/链接：
参考文献标题:Gardos channel antagonists
文献作者:Rigdon,G.C.; McNaughton-Smith,G.A.; Stocker,J.W.(ICAgen,Inc.)
参考来源:EP 1158971; US 6288122; WO 0050026
📄 详细内容
合成路线:The Grignard condensation of 4,4'-difluorobenzophenone (I) with phenylmagnesium bromide (II) in refluxing tert-butyl methyl ether gives the corresponding carbinol (III),which is treated with acetyl chloride in dichloromethane to yield the methyl chloride (IV).Condensation of compound (IV) with copper cyanide by heating at 140 癈,followed by treatment with hot toluene affords 2,2-bis(4-fluorophenyl)-2-phenylacetonitrile (V),which is finally partially hydrolyzed with H2SO4 in refluxing glacial acetic acid.
参考文献标题:ICA-17043
文献作者:Chilman-Blair,K.; Castar,J.; Leeson,P.A.
参考来源:Drugs Fut 2003,28(9),854
产品链接: CAS No. 289656-45-7››