【摘要】 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更多还原

【Abstract】 Objective To modify the synthesis of Benzhydryl 2α-methyl-2β-[(1,2,3- triazol -1-yl)-methyl]penicillanate-1,1-dioxide( Ⅰ ),the key intermediate of β-lactamase inhibitor tazobactam. Methods Ⅰ has been prepared by treating of Benzhydryl 2α-methyl-2β-chloromethyl-penicillanate( Ⅱ )with 1,2,3-triazole, and then oxidized according to the new designed route. Results Reaction conditions of the key step in this route have been optimized and the reaction mechanism was proposed. Conclusion Good yield for the total synthesis of tazobactam would be achieved on the basis of this study.更多还原