2,3,4-三氟硝基苯合成工艺新进展

New progress on synthesis method for 2,3,4-trifluoronitrobenzene

2,3,4-三氟硝基苯是合成氟喹诺酮药物的重要中间体。介绍了4条工艺合成路线,按起始原料分,它们是:1)2,6-二氯苯胺法;2)2,6-硝基苯法;3)2,6-溴苯胺法,4是最近提出的新工艺技术,即以1,2,3-三氯苯作原料,通过硝化、氟化制得到产品。产品纯度达99%,收率为60%,这是一条较有发展前景的工业化合成路线,值得引起关注。

The 2,3,4 - trifluoronitrobenzene is a important pharmaceutical intermediates, for synthesis of fluorquinolone antibacterial agents, such as Tarivid and lamfloxacim etc. At present according to using raw material differences, there are four synthesis methods ： 1 ） by 2,6 - dichlorobenzenamine through Schieman fluorination reaction, nitration reaction and Swarts fluorine exchange reaction ; 2 ） by 2,3 - dichloronitrobenzene as raw material, first steps chlorination, and then through diazotization , fluorination and nitration reaction ;3）by 2,6 -dibromoaniline as raw material through diazotization , fluoric decomposition etc; （4） A new method given for synthesis of 2,3,4 -trifluoronitrobenzene, with the improvement of producing 1,2,3 -trichlorobenzene ,the 1,2,3 -trichlorobenzene was produced 1,2,3 -trifluoro-4 -nitrobenzene via nitration and fluorination,the purity of product was over 99%, and the yield 60%. The method hand the advantages such as the simple reaction steps and esay operation,therefore were introduced especilly in this paper.