盐酸尼莫司汀的合成工艺优化

Improved Synthesis of Nimustine Hydrochloride

目的 对盐酸尼莫司汀的合成工艺进行优化。方法 以2-氯乙胺盐酸盐为起始物料,经取代,亚硝化,缩合,亚硝化,成盐反应生成盐酸尼莫司汀。结果 目标产物经MS、;H NMR等方法进行了结构确证,产品纯度达99.5%以上,总收率35.8%。结论 改进后的工艺反应条件温和,操作简便,适宜工业化生产。

Objective To optimize the synthesis process of nimustine hydrochloride. Methods Starting from 2-chloroethylamine hydrochloride, nimustine hydrochloride was obtained by substitution, nitrosation, condensation,nitrosation and salt formation. Results The structure of nimustine hydrochloride was verified by;H NMR and MS. The purity was above 99.5 %, and the total yield reached 35.8 %. Conclusion The improved process has the advantages of mild reaction condition and simple operation, and is suitable for industrial production.