氟苯咪唑合成工艺优化

Improved Synthesis of Flubendazole

文章旨在优化氟苯咪唑现有生产工艺,优化后的工艺在硝基还原步骤将羰基一并还原为羟基,在环合反应完成后再用双氧水将羟基氧化为羰基。与原有工艺相比,优化后的工艺摒弃了硫化碱还原工艺,更加清洁环保;反应时间缩短,大大提高了生产效率;收率也有5%-8%的提高;纯度可达99.9%。产物进行了核磁波谱和质谱标定,并与标准品进行了高效液相色谱对照。

The paper was aimed at optimizing and improving the synthesis route of flubendazole. In the new synthesis route, the carbanyl group was reduced to hydroxyl together at reduction of nitro and flubendazole was synthesized by oxidation after completion of cyclization. Compared with the original, the new synthesis route was clean and environmental by abandoning the process of sulfide reduction. The production efficiency is improved by shortening the reaction time, the yield was higher 5 %-8 % than before and the purity reached to 99.9 %.The structure was characterized by means of 1HNMR and MS and compared with standard sample by HPLC.