摘要
目的目的2-(2-羟乙基)-3-氨基-4-羧基吡唑是制备硫酸头孢噻利的重要中间体。方法经三步反应合成2-(2-羟乙基)-3-氨基-4-羧基吡唑:以氰乙酸乙酯为起始原料,与原甲酸三乙酯反应得2-氰基-3-乙氧基丙烯酸乙酯,与羟乙肼环合后再水解而得。结果在此条件下,收率可达60.8%。结论本实验方法与其他合成方法比较,具有收率高,操作容易,实用性强等特点,具有一定推广价值。
Abstract
OBJECTIVE synthesize 2-(2-hydroxyemyl)-3-amino-4-carboxylpyrazole,a key intermediate of cefoselis sulfate. METHODS 2-(2-hydroxyethyl)-3-amino-4-carboxylpyrazole was synthesized by a convenient three-step process.Ethyl cyanoacetate as initial raw materials,was reacted with triethyl orthoformate to obtain 2-cycno-3-ethoxyl ethyl acrylate,and then 2-(2-hydroxyethyl)-3-amino-4-carboxylpyrazole was obtained by hydrolyzation after the reaction of cyclization with 2-cycno-3-ethoxylethylacrylate and 2-hydroxyethylhydrazine.RESULTS Under the optimum condition,the yield was over 60.8%. CONCLUSION This experimental technique compares with other synthetic method,has higher receives rate,the operation is easier,more usuable and it has certain promoted value.
关键词
2-(2-羟乙基)-3-氨基-4-羧基吡唑 /
硫酸头孢噻利 /
合成
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Key words
2-(2-hydroxyethyl)-3-amino-4-carboxylpyrazole /
cefoselis sulfate /
synthesis
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郭俊晶;伏广龙;吴庆利;徐沛春.
中间体2-(2-羟乙基)-3-氨基-4-羧基吡唑的合成研究[J]. 中国药学杂志, 2009, 44(10): 796-798
GUO Jun-jing;FU Gung-long;WU Qing-li;XU Pei-chun.
Study on Synthesis of an Intermediate of 2-(2-hydroxyethyl)-3-Amino-4-Carboxylpyrazole [J]. Chinese Pharmaceutical Journal, 2009, 44(10): 796-798
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参考文献
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脚注
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基金
淮海工学院自然基金资助项目(Z2005011)
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