盐酸替扎尼定的合成改进

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-苯并噻二唑,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.

Improved synthesis of tizanidine hydrochloride

Objective:To improve the synthetic way of tizanidine hydrochloride. Methods:Tiza-nidine 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.