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目的改进 β -内酰胺酶抑制剂泰唑巴坦关键中间体 2α -甲基 - 2 β[(1 ,2 ,3-三唑 - 1 -基 ) -甲基 ]青霉烷酸砜二苯甲酯 (Ⅰ )的合成。 方法将 2α-甲基 - 2 β -氯甲基 -青霉烷酸二苯甲酯 (Ⅱ )与 1 ,2 ,3-三唑直接反应 ,再经氧化 ,成功地合成了Ⅰ。 结果对本合成路线中关键步骤的反应条件进行了优化 ,提出了可能的反应机理。 结论该研究结果为提高合成泰唑巴坦的收率奠定了基础
OBJECTIVE To improve the key intermediate of 2 - methyl - 2 β [(1, 2, 3 - triazol - 1 - yl) - methyl] Synthesis of Ester (I). Methods Direct synthesis of 2α-methyl-2β-chloromethyl-penicillanic acid diphenylmethyl ester (Ⅱ) with 1,2,4-triazole and subsequent oxidation followed the successful synthesis of Ⅰ. Results The reaction conditions of the key steps in the synthesis route were optimized and the possible reaction mechanism was proposed. Conclusion The results of this study laid the foundation for the improvement of the yield of synthetic tazobactam