盐酸异波巴胺的合成和工艺改进

Improved synthesis of ibopamine hydrochloride

以 3,4 二甲氧基苯乙胺为原料 ,经N 苄基化、N 甲基化、脱甲基、酯化、脱苄及成盐反应合成盐酸异波巴胺 ,并采用“一锅烩”法合成重要中间体N 苄基 N 甲基 3,4 二甲氧基苯乙胺氢溴酸盐。合成实验中以价格便宜的Ni代替昂贵的Pd/C作催化剂或者采用NaBH4作还原剂 ,脱甲基反应中 ,由加压反应改为常压反应 ,操作简便 ,成本低 ,该工艺适合于工业化生产。产物的结构经红外光谱、质谱、核磁共振氢谱和元素分析确证。

To synthesize ibopamine hydrochloride from 3,4 dimethoxyphenethylamine through reactions of N benzylation, N methylation,esterification,demethylation,debenzylation and salt formation. N benzyl N methyl 3,4 dimethoxyphenethylamine hydrobromide was synthesized via one pot process.In the present invention,cheap Ni was substituted for expensive Pd/C.In addition, N benzyl N methyl 3,4 dimethoxyphenethylamine hydrobromide was obtained by using NaBH 4 as the reductive agent.In the last reaction the normal pressure reaction was substituted for the pressure reaction.The method is a new economical technology with the advantage of lower cost and suitablility for industrial production.The structure of the product was identified by IR,MS, 1H NMR and EA.