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.
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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