头孢西丁钠关键中间体7-α-甲氧基-3-去乙酰基头孢噻吩苄星盐的一步法合成研究  

One-step Synthesis of Cefoxitin Sodium Key Intermediate 7-α-Methoxy-3-deacetyl-cefothiophene Benzathine

作　　者：张宜仲 王金龙 侯仲轲 王兆刚 ZHANG Yi-zhong;WANG Jin-long;HOU Zhong-ke;WANG Zhao-gang(Zhejiang Dongying Pharmaceutical Co., Ltd.;Zhejiang Guobang Pharmaceutical Co., Ltd.)

机构地区：[1]浙江东盈药业有限公司,浙江上虞312369 [2]浙江国邦药业有限公司,浙江上虞312369

出　　处：《精细化工中间体》2023年第2期40-43,共4页Fine Chemical Intermediates

摘　　要：为实现头孢西丁钠关键中间体7-α-甲氧基-3-去乙酰基头孢噻吩苄星盐的一步法合成,以头孢噻吩酸为原料,一锅中进行7-α-甲氧化和3位去乙酰基,不需要拿出中间体,并以溶液状态直接和N,N′-二苄基乙二胺二乙酸成苄星盐得到产品。一步法工艺简化了操作,提高了收率,减少了三废,具有工业化应用前景。The one-step synthesis of the key intermediate of cefoxitin sodium 7-α-methoxy-3-deacetylcefothiophene benzathine was studied.Using cefalotin acid as the raw material,conduct 7-α-methoxidation and 3-position deacetylation,without taking out the intermediate,and directly reacting with DBED in solution state to obtain the product.The process is simplified,the yield is improved,and the three wastes are reduced,which has a prospect of industrial application.

关 键 词：头孢噻吩酸 7-α-甲氧基-3-去乙酰基头孢噻吩苄星盐 一步法合成 头孢西丁钠 

分 类 号：TQ465[化学工程—制药化工]