5-氨基-1-羟乙基吡唑的合成

Synthesis of 5-amino-1-hydroxyethyl pyrazole

目的合成5-氨基-1-羟乙基吡唑。方法原甲酸三乙酯与氰乙酸乙酯缩合,然后和羟乙基肼经环合、水解等一锅法合成5-氨基吡唑-4-甲酸,然后在亚硫酸钠存在条件下加热脱羧得到5-氨基-1-羟乙基吡唑。结果合成得到5-氨基-1-羟乙基吡唑。结论该工艺路线同现有文献相比,不仅总产率较高,而且简化了合成工艺,节省了原料和成本,减少对环境的污染。

OBJECTIVE To synthesis 5- amino- 1 - hydroxyethyl pyrqazole. METHODS 5- amino- 1 - hydroxyethyl pyrazole-4-carboylic acid was synthesized through condensation of ethyl cyanoacetate and triethyl orthoformate followed by one-pot methodology of cyclization,hydolysis. 5-amino-1-hydroxyethylpyrazole was obtained from thermal decarboxylation of 5- amino - 1 - hydroxyethylpyra zole - 4 - carboxylic acid at the present of sodium sulfite. RESULTS 5 - amino - 1 - hydroxyethyl pyrazole was successfully synthesized. CONCLUSION It was a convenient and efficient method in high yield and high purities comparison with literature.