3-溴甲基头孢烯酸二苯甲酯S-氧化物的合成

SYNTHESIS OF 3-BROMOMETHYLCEPHEMBEN- ZHYDRYL ESTER S-OXIDE

3-溴甲基头孢烯酸二苯甲酯S-氧化物是研制C_(10)-取代头孢菌素的关键中间体。本文对合成比中间体的方法进行了研究。实验采用青霉素扩环路线,以(牙卡)基青霉素为原料经由去乙酰氧头孢烯酸及其二苯甲酯S-氧化物转化成3-溴甲基头孢烯酸二苯甲酯S-氧化物,总收率为40—50％。

3-Eromomethylcephembenzhydryl ester S-oxide is an important intermediate in the preparation of C_(10)-substituted cephalosporins. Synthetic method for this compound was studied. Eenzylpenicillin was employed as starting meterial and converted to 3-bromomethylcephembenzhydryl ester S-oxide through the deace- toxycephem and its benzhydryl ester S-oxide by ring expansion method. The overall yield is 40-50%.