他唑巴坦的合成

Synthesis of Tazobactam

以 2 β-氯甲基青霉烷酸二苯甲酯为起始原料 ,经叠氮化、氧化后 ,用乙炔成三唑环 ,再用间甲苯酚脱羧基保护基制得新型 β-内酰胺酶抑制剂他唑巴坦 ,总收率 2 8%。

Tazobactam, a β-lactamase inhibitor, was synthesized from benzhydryl 2β-chloromethyl 2α-methylpenam-3α-carboxylate by azidation, oxidation, cyclization with acetylene to form triazole, and then deprotection with m-cresol in an overall yield of 28%.