合成路线:The condensation of 3-pyridincarboxaldehyde (I) with diethyl malonate (II) by means of piperidine in refluxing benzene gives diethyl (3-pyridyl)methylenemalonate (III),which by reaction with dimethylamine (A) in ether is converted into diethyl alpha-dimethylamino-(3-pyridyl)methylmalonate (IV).The reduction of (IV) with LiAlH4 in THF affords 2-[alpha-dimethylamino-(3-pyridyl)methyl]-1,3-propanediol (V),which is finally cyclized with paraformaldehyde by means of boron trifluoride ethearate in acetonitrile.(1-3)
参考文献标题:Doxpicomine hydrochloride
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.
参考来源:Drugs Fut 1981,6(9),548
合成路线:The condensation of 3-pyridincarboxaldehyde (I) with diethyl malonate (II) by means of piperidine in refluxing benzene gives diethyl (3-pyridyl)methylenemalonate (III),which by reaction with dimethylamine (A) in ether is converted into diethyl alpha-dimethylamino-(3-pyridyl)methylmalonate (IV).The reduction of (IV) with LiAlH4 in THF affords 2-[alpha-dimethylamino-(3-pyridyl)methyl]-1,3-propanediol (V),which is finally cyclized with paraformaldehyde by means of boron trifluoride ethearate in acetonitrile.(1-3)
参考文献标题:
文献作者:Booher,R.N.(Eli Lilly and Company)
参考来源:US 3962269
合成路线:The condensation of 3-pyridincarboxaldehyde (I) with diethyl malonate (II) by means of piperidine in refluxing benzene gives diethyl (3-pyridyl)methylenemalonate (III),which by reaction with dimethylamine (A) in ether is converted into diethyl alpha-dimethylamino-(3-pyridyl)methylmalonate (IV).The reduction of (IV) with LiAlH4 in THF affords 2-[alpha-dimethylamino-(3-pyridyl)methyl]-1,3-propanediol (V),which is finally cyclized with paraformaldehyde by means of boron trifluoride ethearate in acetonitrile.(1-3)
参考文献标题:
文献作者:Booher,R.N.(Eli Lilly and Company)
参考来源:US 3905987
产品链接: CAS No. 69494-04-8›› 产品链接: CAS No.62904-71-6››