【摘要】 介绍了合成2,3,4,5-四氟苯甲酸的8条工艺路线,按采用主要原料来分,它包括:四氯苯酐法,四氟苯甲醇法,邻苯二腈法,四氟苯法,八氯萘法,N-苯基四氯邻苯二甲酰亚胺法等。对其中四氯苯酐法和N-苯基四氯邻苯二甲酰亚胺法,由于原料易得,操作条件适宜,容易工业化等原因作了重点叙述。合成步骤一般采用缩合、氟化、开环、脱羧和水解等反应合成2,3,4,5-四氟苯甲酸。2,3,4,5-四氟苯甲酸是一种重要的医药中间体,尤其是合成第3、4代喹诺酮抗菌药物的重要原料或中间体,如合成:洛美沙星、司氟沙星、氟罗沙星、氧氟沙星、左氧氟沙星和芦氟沙星等。从发展趋势看,世界抗菌药物市场正在由头孢菌素向喹诺酮药物转移,所以,开发2,3,4,5-四氟苯甲酸具有璀璨的前景。更多还原

【Abstract】 In this paper, eight techniques for synthesis of 2,3,4,5-Tetrafluorobenzoic Acid were summarized in detail. The synthetic methods are mainly comprising: Starting raw material with ①1,2,3,4-tetrachloro-phthalicanhydride,②O-phthalodinitrile,③N-phenyltetrachlorophthalimidine, ④Otachloro-naphthalene, ⑤1,2,3,4-tetrafluoro-ben-zene, ⑥2,3,4,5-tetrafluoro-benhydrol etc. therein: ①with starting 1,2,3,4-tetrachlorophthalicanhydride and aniline via condensation reaction, fluoridization reaction, opening-ring, reaction decarboxylation reaction and hydrolysis reaction; other wise with③starting N-phenyhertrochlorophthalimidine via fluoridization reaction, opening-ring reaction, decarboxylation reaction and hydrolysis reaction were described emphatically. This two methods is the hot spot of development at home and abooad,In comparison with existing synthesis methods,this process is characterized by plenty raw material source, simple precess, and less "three waste". The syntheyic route is suitable for commercial production as its mild reaction condition. 2,3,4,5 -Tetrafluorobenzoic Acid chief use for preparation of antibacterial agents of quinolone, such as Lomefloxacin, Sparfloxacin, fleroxacin,ofloxacin,Levofloxacin and Rufloxacin etc. which is characterized by little side-effect,high efficientand lower toxicity. Quinolone drug was synthesis from 2,3,4,5 -Tetrafluorobenzoic acid annual sales over US dollor hundred million, so that they have good social and economic benefits. In the field of medicines for antibiotic therapy, the global market focus is transferring from cephalosporin to fluoroquinolones.更多还原