Synthesis of Tazobactam,β-Lactamase Inhibitor

β-内酰胺酶抑制剂他唑巴坦的合成(英文)

Tazobactam,β lactamase inhibitor, was synthesized from 6 aminopenicillanic acid through eleven steps, including diazotization, bromination, oxidation, chlorization, cyclization, deprotection and so on. The designed route was examined, particularly the azide substitution and cyclization. In the latter reaction, vinyl acetic ester was employed in place of acetylene.

以 6 氨基青霉烷酸 (6 APA)为原料 ,经重氮化、溴化、氧化、氯化、叠氮取代、环合、脱保护等 11步反应合成了 β 内酰胺酶抑制剂他唑巴坦 (Tazobactam) ,并对叠氮取代和环合进行了研究 。