广谱抗菌剂普卢利沙星的合成

Synthesis of Broad-spectrum Antimicrobial Prulifloxacin

以 3, 4- 二氟苯胺为起始原料,经过加成、硫代缩环、环合、缩合等一系列反应,最后得产品普卢利沙星;经过元素分析,产品的元素组成为C21H20FN3O6S,精制品与对照品的EA、UV、IR、NMR、MS、DSC、TG和X -ray测定结果一致,两者为同一结构、同一晶型化合物;产品的纯度达到 99. 0%以上,改进后的工艺更适合工业化生产。

Using 3,4-difluoroaniline as raw material, prulifloxacin with purity of 99.0% was synthesized through a range of reactions namely addition, thionation, cyclization and condensation reactions. Its composition was confirmed as C 21H 20FN 3O 6S by the elemental analysis. The refined product is identical with the standard sample in the characterization results of EA、UV、IR、NMR、MS、DSC、TG and X-ray, it indicated that they have the same structure and crystal form. The improved technology is much suitable for commercial production.