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托吡酯合成工艺研究
引用本文:陈 滔,韩建萍,张村子,吕丽娟.托吡酯合成工艺研究[J].医学教育探索,2012,27(5):449-450.
作者姓名:陈 滔  韩建萍  张村子  吕丽娟
作者单位:天津泰普药品科技发展有限公司,天津 300193
摘    要:目的 合成托吡酯并对工艺进行研究。方法 以D-果糖为起始原料,在浓硫酸的催化下,与丙酮缩合生成双丙酮果糖,再同氯磺酸异氰酸酯反应采用“一锅法”制备,得到托吡酯。结果 本工艺总收率为43.3%。结论 工艺改进后,简化了操作过程,提高了托吡酯的收率。

关 键 词:托吡酯  D-果糖  氯磺酸异氰酸酯  合成

Synthesis of topiramate
Abstract:Objective To synthesize topiramate and research the synthetic process. Methods Catalyzed by concentrated sulfuric acid, D-fructopyranose was used as the initial raw material, then condensation of D-fructopyranose with acetone to synthesize 2,3,4,5-bis-O-(1-methylethylidene)-D-fructopyranose. The topiramate was produced by reaction between 2,3,4,5-bis-O-(1- methylethylidene)-D-fructopyranose and chlorosulfonyl isocyanate via one pot method. Results The total yield by the synthetic process was 43.3%. Conclusion After the process improvement, the operating process is simplified and the yield of topiramate is improved.
Keywords:topiramate  D-fructopyranose  chlorosulfonyl isocyanate  synthesis
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