泰唑巴坦关键中间体的合成研究

目的　改进β-内酰胺酶抑制剂泰唑巴坦关键中间体2α-甲基-2β(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-2β-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。

Study on Synthesis of Key Intermediate of Tazobactam

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 in-hibitor 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 designedroute. Results Reaction conditions of the key step in this route have been optimized and the reactionmechanism was proposed. Conclusion Good yield for the total synthesis of tazobactam would beachieved on the basis of this study.