2-乙氧基-N-(4-甲基-2-丙基-1H-咪唑基-1)-苯甲酰胺的合成  

Synthesis of 2-Ethoxy-N-(4-methyl-2-propyl-1H-imidazol-1-yl)benzamide

作　　者：俞颖慧[1] 许煦[2] 段梅莉[1] 罗晓燕[1] 冀亚飞[1] 

机构地区：[1]华东理工大学药学院,上海200237 [2]华东理工大学化工学院,上海200237

出　　处：《合成化学》2008年第5期603-605,共3页Chinese Journal of Synthetic Chemistry

摘　　要：2-乙氧基苯甲酸甲酯与水合肼发生肼解反应生成2-甲氧基苯甲酰肼(1);1与丁亚氨酸乙酯盐酸盐进行二次肼解反应制得2-乙氧基-N′-(1-亚胺丁基)苯甲酰肼盐酸盐(3);3与氯丙酮环化合成了2-乙氧基-N-(4-甲基-2-丙基-1H-咪唑基-1-)苯甲酰胺(合成伐地那非的关键中间体),总收率48%,其结构经1H NMR和MS确证。A key intermediate of vardenafil, 2-ethoxy-N-（4-methyl-2-propyl-lH-imidazol-1-yl） benzamide（4） in an overall yield of 48%, was synthesized by a three-step reaction. Hydrazinolysis of methyl 2-ethoxybenzoate with hydrazine hydrate was first carried out to obtain 2-methoxybenzol hydrazinc（1） ; hydrazinolysis was then performed between ethyl butyrimidate hydrochloride and 1 to produce 2-ethoxy-N＇-（1-iminobutyl） benzohydrazide hydrochloride （3） ; 3 was finally eyclized With ehloroaeetone to give 4. The structures were confirmed by ^1H NMR nnd MS.

关 键 词：肼解反应 伐地那非 苯甲酰胺 合成 

分 类 号：O625.52[理学—有机化学] R914.5[理学—化学]