β-内酰胺酶抑制剂他唑巴坦的合成

摘要

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,成功地以醋酸乙烯酯代替乙炔进行了环合.%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.