4-(4-吗啉)哌啶盐酸盐的合成

Synthesis of 4-(Morpholin-4-yl)piperidine Dihydrochloride

4-甲酸乙酯哌啶与溴苄反应,再经酰胺化和氨化反应制得关键中间体4-氨基-1-苄基哌啶(5);5与2,2-二溴二乙醚经环化反应制得N-苄基-4-(4-吗啉)哌啶,再经成盐,加氢合成了4-(4-吗啉)哌啶盐酸盐(1,总收率24.9%),1的结构经1HNMR,IR和GC-MS确认。

A key intermediate,4-amino-1-benzylpiperidine（5）,was prepared by the reaction of ethyl isonipecotate with benzyl bromide,then acylamination and ammonification.5 reacted with bis（2-bromoethyl）ether,and then by salt-forming and hydrogenation to obtain 4-（morpholin-4-yl）piperidine（1）in total yield of 24.9%.The structure of 1 was confirmed by 1H NMR,IR and GC-MS.