喹诺酮类抗菌素双氟哌酸的合成与研究

Synthesis and Study of Antibacterial Quinolone of Diflonacin

提出了以 2 ,4-二氯 -5 -氟苯甲酰乙酸甲酯和原甲酸三甲酯为主要原料 ,乙酸酐为催化剂 ,经氨化、环化、水解和缩合制备喹诺酮类抗菌素双氟哌酸的合成路线。利用元素分析、质谱、红外光谱 ,核磁共振氢谱对双氟哌酸的结构进行表征。实验结果表明 :采用本文提出的合成路线制备双氟哌酸 ,其纯度高 。

The title compound can be prepared with the stocks of 2,4-dichloro-5-fluorobenzoyl acetic formate and trimethylorthoformate and acetic anhydride as catalyst at moderate condition by amination , cyclization, hydrolysis and condensation. The element analysis, IR, MS and HNMR data were determined for the title compound and were evaluated as consistent with the indicated structure. The purity of diflonacin was higher and condition of the process was controlled well.