青霉烷酸对甲氧基苄酯-1α-亚砜的合成方法改进

An Improved Synthesis of p Methoxybenzyl Penicillanate-1α-oxide

以 6 APA为起始原料 ,经溴化得 6 ,6 二溴青霉烷酸 ,用 11%～ 13 %的过氧乙酸氧化 ,所得的氧化产物 3以固体形式直接从溶液中析出 ,3以对甲氧基溴苄进行羧基保护 ,经还原合成了 β 内酰胺酶抑制剂他唑巴坦的关键中间体青霉烷酸对甲氧基苄酯 1α 亚砜 1。本方法操作简便 ,价格低廉 ,实施安全 。

Dibromopenicillanic acid was oxidized with 11%～13% peracetic acid,and its oxiding product could precipitate directly from the solution.The key intermediate for β lactamase inhibitor BL P2013、Ro48 1220 and tazobactam p methoxybenzyl penicillanate 1α oxide was synthesized by the convenient,cheap and safe method,which fitted in with production on a scale.