盐酸替扎尼定的合成改进  

Improved synthesis of tizanidine hydrochloride

作　　者：吴贝[1] 沈怡[1] 周鸣强[1] 邓勇[1] 

机构地区：[1]四川大学华西药学院,成都610041

出　　处：《中国新药杂志》2006年第8期621-623,共3页Chinese Journal of New Drugs

摘　　要：目的:改进盐酸替扎尼的合成路线。方法:以4-氯-2-硝基苯胺为起始原料,经还原反应和环合反应得5-氯-2,1,3-苯并噻二唑,再经硝化反应,还原反应得5-氯-4氨基-2,1,3-苯井噻二唑,与N-乙酰基-2-咪唑烷酮发生缩合反应后,再经醇解反应、成盐反应等步骤制得盐酸替扎尼定。结果:目标化合物的结构经红外光谱、核磁共振氢谱、核磁共振碳谱、质谱及元素分析确证。总收率52．4％。结论:本改进合成方法反应条件温和,操作简便。Objective ：To improve the synthetic way of tizanidine hydrochloride. Methods： Tizanidine hydrochloride was synthesized using 4-chloro-2-nitroaniline as a starting material via several steps, including reduction with hydrazine/Fe-C, cyclization, nitrition and reduction of nitro group with Fe/HOAc, condensation of 5-chloro-4-amino-2, 1 , 3-benzothiadiazole with N-acetyl-2-imidazolidinone, alcoholysis and salification. Results：Total yield of the target compound was 52.4%. The structure of the target compound was confirmed by IR,^1H-NMR, ^13C-NMR, MS and element analysis. Conclusion： This improved synthetic procedure was mild and easily manipulated.

关 键 词：盐酸替扎尼定 肌肉松弛药 药物合成 

分 类 号：R971.8[医药卫生—药品] R914.5[医药卫生—药学]