| 正交试验法优选穿心莲内酯硫酸酯化反应工艺 |
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| 引用本文： | 许卉,王功富,刘珂,付颖颖,杨小玲. 正交试验法优选穿心莲内酯硫酸酯化反应工艺[J]. 化学研究与应用, 2008, 20(11) |
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| 作者姓名： | 许卉 王功富 刘珂 付颖颖 杨小玲 |
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| 作者单位： | 烟台大学药学院,山东,烟台,264005;江西青峰药业有限公司,江西,赣州,341000 |
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| 摘 要： | 硫酸酯化反应以分子结构中的羟基为反应位点,向有机分子中引入硫酸酯基,是一种有效改善天然产物水溶性的结构修饰途径[1]。有些药物因水溶性差,致使其在临床应用中存在一些问题,如生物利用度不高,服用量大,制成的片剂或胶囊体内吸收缓慢等。这类化合物经硫酸酯化后不但可以增加
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| 关 键 词： | 穿心莲内酯 硫酸酯化反应 正交试验 综合评分法 |
Optimal technical study on sulfonation of andrographolide by orthogonal-design experiment |
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| XU Hui,WANG Gong-fu,LIU Ke,FU Ying-ying,YANG Xiao-ling. Optimal technical study on sulfonation of andrographolide by orthogonal-design experiment[J]. Chemical Research and Application, 2008, 20(11) |
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| Authors: | XU Hui WANG Gong-fu LIU Ke FU Ying-ying YANG Xiao-ling |
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| Abstract: | An orthogonal-design experiment with the type of L9(34) is applied to optimize the condition for sulfonation of andrographolide with concentrated sulfuric acid.The optimal sulfonation condition is established by general analysis of reacting percentage of sulfonation agent and the yield of main aim product with multi-target grading method.The multi-target grade is significantly affected by the weight ratio of concentrated sulfuric acid to andrographolide,whereas reaction time and concentration of the alkali used for neutralization have insignificant effect.The optimal condition is established as concentrated sulfuric acid reacting with half weight of andrographolide for 72 h and then neutralized by sodium hydroxide with a weight concentration of 30%. |
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| Keywords: | andrographolide sulfonation orthogonal-design experiment multi-target grading method |
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