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德国Hoechst公司于1983年报道了代号为HR810的新的头孢菌素,是一种新型的氨基噻唑类衍生物,命名为cefpirome(CPR,头孢匹罗),随后法国Roussel参与了共同开发,日本也申请进行开发,美国等即将完成Ⅲ期临床研究。CPR的主要特点为广谱、高效、耐酶(均优于第三代头孢菌素)。本文对本品有关的研究进展综述如下。一、化学合成及结构特点合成路线有两条:(1)用2,3-环戊烯并吡啶(1)直接置换头孢噻肟(CTX)的3′-乙酰氧基制得本品(2)。(2)用7-氨基-[3-(2,3-环戊烯并吡啶)甲基-7-头孢-3-烯-4羧酸
The German company Hoechst reported in 1983 a new cephalosporin, codenamed HR810, a new aminothiazole derivative named cefpirome (CPR, cefpirome), followed by Roussel in France for joint development and Japan Apply for development, the United States and other upcoming phase Ⅲ clinical studies. The main features of CPR are broad spectrum, high efficiency, resistance to enzymes (all superior to the third generation cephalosporins). This article on the product-related research are summarized below. First, the chemical synthesis and structural characteristics of the synthetic route has two: (1) 2,3-cyclopentenopyridine (1) direct replacement of cefotaxime (CTX) 3’-acetoxy this product (2 ). (2) Using 7-amino- [3- (2,3-cyclopenopyridine) methyl-7-ceph-3-ene-4-carboxylic acid