Norzimelidine, Botiacrine, CPP-199, A-24356
诺美立定Chemical Name: N-[3-(4-Bromophenyl)-3-(3-pyridinyl)-2(Z)-propenyl]-N-methylamine
CAS No. 60324-59-6
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:The condensation of 4-bromophenyl-3-pyridyl ketone (I) with ethyl bromoacetate (II) by means of Zn in refluxing benzene gives ethyl 3-hydroxy-3-(3-pyridyl)-3-(4-bromophenyl)propionate (III),which is reduced with LiAlH4 in refluxing ethyl ether yielding 1-(3-pyridyl)-1-(4-bromophenyl)propane-1,3-diol (IV).Finally this compound is treated first with PBr3 and HBr in refluxing acetone,and then with methylamine (V) at 110 C in a pressure vessel
合成路线:The condensation of 4-bromophenyl-3-pyridyl ketone (I) with ethyl bromoacetate (II) by means of Zn in refluxing benzene gives ethyl 3-hydroxy-3-(3-pyridyl)-3-(4-bromophenyl)propionate (III),which is converted into the corresponding methylamide (VI) by treatment with methylamine (V) in ethanol.This compound is reduced with NaBH4 in THF yielding 3-(3-pyridyl)-3-(4-bromophenyl)-3-hydroxy-N-methylpropylamine (VII),which is finally dehydrated by treatment with 50% H2SO4 at 110 C
📌 参考资料/链接：
参考文献标题:Nomelidine
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.; Sweetman,A.J.
参考来源:Drugs Fut 1979,4(12),885
📄 详细内容
合成路线:The condensation of 4-bromophenyl-3-pyridyl ketone (I) with ethyl bromoacetate (II) by means of Zn in refluxing benzene gives ethyl 3-hydroxy-3-(3-pyridyl)-3-(4-bromophenyl)propionate (III),which is reduced with LiAlH4 in refluxing ethyl ether yielding 1-(3-pyridyl)-1-(4-bromophenyl)propane-1,3-diol (IV).Finally this compound is treated first with PBr3 and HBr in refluxing acetone,and then with methylamine (V) at 110 C in a pressure vessel
合成路线:The condensation of 4-bromophenyl-3-pyridyl ketone (I) with ethyl bromoacetate (II) by means of Zn in refluxing benzene gives ethyl 3-hydroxy-3-(3-pyridyl)-3-(4-bromophenyl)propionate (III),which is converted into the corresponding methylamide (VI) by treatment with methylamine (V) in ethanol.This compound is reduced with NaBH4 in THF yielding 3-(3-pyridyl)-3-(4-bromophenyl)-3-hydroxy-N-methylpropylamine (VII),which is finally dehydrated by treatment with 50% H2SO4 at 110 C
参考文献标题:
文献作者:Carlsson,P.A.E.; et al.(Astra L鋕emedel AB)
参考来源:BE 835802; DD 122528; DE 2550005; FR 2291751; JP 7676278; NL 7513648; ZA 7506893
产品链接: CAS No. 60324-59-6››