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托吡酯合成工艺研究 被引量:2

Synthesis of topiramate
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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。 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-(1methylethylidene)-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.
出处 《现代药物与临床》 CAS 2012年第5期449-450,共2页 Drugs & Clinic
关键词 托吡酯 D-果糖 氯磺酸异氰酸酯 合成 topiramate D-fructopyranose chlorosulfonyl isocyanate synthesis
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  • 1Maryanoff B E, Nortey S O, Gardocki J F, et al. Anticonvulsant O-alkyl sulfamates. 2,3:4,5-bis-O-(1- rhethylethylidene)-beta-D-fructopyranose sulfamate and related compounds [J]. J Med Chem, 1987, 30(5): 880- 887.
  • 2卓超,程国候.托吡酯的合成[J].中国医药工业杂志,1999,30(11):486-487. 被引量:6
  • 3马里安诺夫 C A,施科特 L,索吉 K L.一种制备氨基磺酸酯衍生物的改进方法[P].中国:92111591,1997-09-10.
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