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莫吉司坦的合成工艺的改进
引用本文:黄剑,陈年根,钟霞.莫吉司坦的合成工艺的改进[J].海南医学院学报,2011,17(8):1015-1016,1020.
作者姓名:黄剑  陈年根  钟霞
作者单位:海南医学院药学院药物化学教研室,海南海口,571101
基金项目:海南省科技厅基金资助项目(081012)~~
摘    要:目的:合成莫吉司坦,并对其合成工艺进行改进.方法:以愈创木酚甘油醚(2)为起始原料,经高碘酸氧化成醛,简单分离提取后与半胱胺盐酸盐环合得1,3-四氢噻唑,最后在脱水剂的作用下与丙二酸单乙酯进行酰胺化而制得目标化合物.结果:总收率为72.0%,结构经1H-NMR和熔点确证.结论:改进后的工艺操作简便易行,同时最后一步酰胺...

关 键 词:莫吉司坦  愈创木酚甘油醚  丙二酸单乙酯  丙二酸单乙酯酰氯

Improvement in synthesis process of Moguisteine
HUANG Jian,CHEN Nian-gen,ZHONG Xia.Improvement in synthesis process of Moguisteine[J].Journal of Hainan Medical College,2011,17(8):1015-1016,1020.
Authors:HUANG Jian  CHEN Nian-gen  ZHONG Xia
Institution:HUANG Jian,CHEN Nian-gen,ZHONG Xia (Department of Pharmaceutical Chemistry,Pharmacy Faculty,Hainan Medical University,Haikou 57,China)
Abstract:Objective: To improve the synthesis process of Moguisteine.Methods: The target compound was synthesized with guaifenesin as starting material.It was oxidized by periodic acid.1,3-tetrahydrothiazole was obtained by cyclization with cysteamine hydrochloride after simple extraction,and then amidated with monoethyl malonic acid under the reaction of dehydrating agent.Results: The overall yield was 72.0%,and the structure of final compoud was confirmed by 1H-NMR and melting point.Conclusions: The process was sim...
Keywords:Moguisteine  Guaifenesin[Monoethyl malonic acid[Ethyl malonyl chloride  
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