摘要
C_3-氯代头孢烯酸类衍生物头孢克洛2001年在美国的销售额超过8千万美元,位居抗生素类药物销售额第二位。而我国由于没有母核供应,只能进口国外原料药进行分装。C_3-氯代头孢母核的合成方法有两种:青霉素扩环和7-ACA改造。青霉素扩环法操作复杂、收率低、难以实现工业化。文章详细分析了以7-ACA为原料合成C_3氯代头孢母核的各步反应。
In 2001 , the sales of
cefaclor ( No. 2 in the sales of antibiot-
ics) ,a derivative of 3-chloro cephalospo-
rin nucleus, was more than $ 80 mil-
lion. Because there is no supply of 3-
chloro cephalosporin nucleus, China has
to import cefaclor in bulk and pack to
sell. There are two preparation methods
of 3-chloro cephalosporin nucleus: ring
enlargement of penicillin and rebuilding
of 7-ACA. However, ring enlargement of
penicillin is difficult to be commercial-
ized due to complex steps and low yield.
This article analyzes every step in syn-
thesis of 3-chloro cephalosporin nucleus
based on 7-ACA.
出处
《精细与专用化学品》
CAS
2003年第8期16-19,共4页
Fine and Specialty Chemicals
