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头孢硫脒合成工艺改进
引用本文:王洪林,李立威. 头孢硫脒合成工艺改进[J]. 中国现代应用药学, 2010, 0(2): 126-127,180
作者姓名:王洪林  李立威
作者单位:荆楚理工学院化工与药学院,湖北荆门448000
摘    要:目的研究头孢硫脒的合成工艺,使之适合工业化生产,并提高收率。方法以7-ACA为原料,与溴乙酰溴在低温、碱性条件下经C-7位上的氨基酰化,再同侧链二异丙基硫脲缩合制得头孢硫脒。结果总收率由45%提高到62%,产物经IR,MS,1H-NMR确证结构。结论改进后的工艺过程大为简化,总收率得到了提高,适合于工业化生产。

关 键 词:头孢硫脒  头孢菌素  合成

Improved Synthesis Process of Cefathiamidine
WANG Honglin,LI Liwei. Improved Synthesis Process of Cefathiamidine[J]. The Chinese Journal of Modern Applied Pharmacy, 2010, 0(2): 126-127,180
Authors:WANG Honglin  LI Liwei
Affiliation:(Chemical and Pharmaceutical Sciences,Jingchu University of Technology,Jingmen 448000,China)
Abstract:OBJECTIVE To synthesize the title compound and improve process to make it suitable for industrial production,and increase yield.METHODS Cefathiamidine was synthesized from 7-ACA as starting material,acylated by bromoacetyl bromide at C-7 position in a low temperature and alkaline condition,and then condensed by side chain diisopropylthiourea.RESULTS The overall yield was increased from 45% to 62%,the structure of product was confirmed by IR,MS,and 1H-NMR.CONCLUSION The improved process was greatly simplified,with a total yield improved,and suitable for industrial production.
Keywords:cefathiamidine  cephalosporin  synthesis
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