| 5-氨基-1-（2-羟乙基）吡唑的合成工艺优化 |
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| 引用本文： | 王贵军.5-氨基-1-（2-羟乙基）吡唑的合成工艺优化[J].河北化工,2011,34(7):9-10. |
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| 作者姓名： | 王贵军 |
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| 作者单位： | 华北制药股份有限公司新药研究中心,微生物药物国家工程研究中心,河北省工业微生物代谢工程技术研究中心,河北石家庄050015 |
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| 摘 要： | 5-氨基-1-（2-羟乙基）吡唑是第4代硫酸头孢噻利的C-3位侧链。用乙氧亚甲基氰乙酸乙酯和羟乙基肼为原料,经环合、水解等一锅反应合成5-氨基-1-（2-羟乙基）-4-甲酸吡唑,然后加热脱羧得到5-氨基-1-（2-羟乙基）吡唑。分析了反应原理,优化了合成条件,提高了收率,减少了副产物的产生。
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| 关 键 词： | 头孢噻利 5-氨基-1-（2-羟乙基）吡唑 乙氧亚甲基氰乙酸乙酯 羟乙基肼 合成 |
Process Optimization for the Synthesis of 5-Amino-1-(2-hydroxyethyl) pyrazole |
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| WANG Gui-jun.Process Optimization for the Synthesis of 5-Amino-1-(2-hydroxyethyl) pyrazole[J].Hebei Chemical Engineering and Industry,2011,34(7):9-10. |
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| Authors: | WANG Gui-jun |
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| Affiliation: | WANG Gui-jun(NCPC New Drugs R & D Center,National Engineering Research Center of Microbial Medicine,Hebei Industry Microbial Metabolic Engineering & Technology Research Center,Shijiazhuang 050015,China) |
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| Abstract: | 5-Amino-1-(2-hydroxyethyl) pyrazole is the C-3 side-chain of cefoselis sulfate.5-Amino-1-(2-hydroxyethyl)-4-formic acid pyrazole was prepared with 2-cyano-3-ethoxyl-ethyl anrylate and 2-hydroxyethyl hydrazine as raw materials,by one-pot methodology of cyclization,hydrolysis and acidification.5-Amino-1-(2-hydroxyethyl) pyrazole was obtained by thermal decarboxylation of 5-Amino-1-(2-hydroxyethyl)-4-formic acid pyrazole.To analyze the reaction mechanism and influential factors,It’s a convenient and efficient method in high yield and high purities comparison with literature. |
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| Keywords: | cefoselis 5-amino-1-(2-hydroxyethyl) pyrazole 2-cyano-3-ethoxyl-ethylanrylate 2-hydroxyethyl hydrazine synthesis |
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