盐酸奈福泮合成工艺的改进

Improved synthesis of nefopam hydrochloride

目的提高收率,降低成本。方法以邻苯甲酰苯甲酸为起始原料,经三氯化磷酰化,N-甲基乙醇胺胺化,三氯化磷氯化,硼氢化钾还原,然后和氯化氢反应得盐酸奈福泮。结果收率提高了15%,原料成本每公斤降低了50元左右。结论改进后的工艺路线科学、合理,是一个较好的工艺合成路线。

OBJECTIVE Raise production rate and lower cost. METHODS An improved synthesis of nefopam hydrochloride [Ⅲ] is described. Acylation of starting material o-benzoyl benzoic acid with phosphorus trichloride, amination with N-methyl ethnolamine, chloration with phosphorus trichloride, reduction with potassium borohydride, than reaction by hydrogen chloride gave nefopam hydrochloride. RESULTS Production rate increase by 15 per cent and cost of raw material reduce 50 yuan per kilogram. CONCLUSION This synthetic revised process is scientific and reasonable after improvement.