Ⅲ类抗心律失常药多非利特的合成

Synthesis of class Ⅲ antiarrhythmic agent Dofetilide

目的 合成多非利特并改进合成工艺。方法 以对硝基苯酚为起始原料 ,经取代、还原、甲磺酰化等反应制得 4 (β 溴乙氧基 )甲磺酰苯胺 (5 ) ;以对氨基苯乙醇为起始原料 ,经甲磺酰化、甲氨化等反应制得 4 [β (甲氨基 )乙基 ]甲磺酰苯胺 (8) ,再与5经取代反应制得多非利特。结果 所得产物经元素分析、紫外光谱、红外光谱、核磁共振谱及质谱等确证了结构。

OBJECTIVE To synthesize dofetilide and optimize the process. METHOD Dofetilide was synthesized by steps of reaction (substitution ,reduction, methylsulfonylation and methylammoniation, etc) from p-nitrophenol and p-amino phenethyl alcohol. RESULTS Chemical structure of Dofetilide was conformed by element analysis, UV ,IR ,()~1HNMR, and ESI-MS etc. CONCLUSION This synthetic method was feasible.