罗沙替丁衍生物的合成  

Synthesis of Roxatidine Derivatives

作　　者：张辉[1] 张倩云[2] 林莉[1] 程卯生[3] 

机构地区：[1]沈阳医学院化学教研室,辽宁沈阳110034 [2]中国医科大学公共卫生学院,辽宁沈阳110001 [3]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《合成化学》2008年第3期364-366,共3页Chinese Journal of Synthetic Chemistry

摘　　要：以间羟基苯甲醛为原料,经3步反应合成了N-{3-[3-(1-甲基哌啶)苯氧基]丙基}氯乙酰胺(3);3与乙酸钾反应得到H2-受体拮抗剂罗沙替丁乙酸酯盐酸盐;3与伯胺反应合成了4个罗沙替丁的衍生物,再与草酸成盐得对应的草酸盐,其结构经1H NMR,IR和MS表征。N- { 3- [ 3- （ 1 -methylpiperidine） phenoxy ] propyl } chloroacetamide （ 3 ） was synthesized by a three-step reaction from m-hydroxyl-benzaldehyde. Salt of roxatidine acetic ester with hydrochloric acid was prepared by the reaction of 3 with AcOK. Four roxatidine derivatives were synthesized by the reaction of 3 with primary amine and then with oxalic acid to obtain thier salts. The structures were confirmed by ^1H NMR, IR and MS.

关 键 词：罗沙替丁 H2-受体拮抗剂 苯甲醛 药物合成 

分 类 号：O626.24[理学—有机化学] R914.5[理学—化学]