2,3,4,5—四氟苯甲酸的合成工艺进展与展望  

Progress in synthetic process and developwent trend of 2,3,4,5 -tetrafluorobenzoic acid

作　　者：徐兆瑜[1] 

机构地区：[1]安徽省化工研究院,安徽合肥230041

出　　处：《化工科技市场》2006年第7期30-33,共4页Chemical Technology Market

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。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 - phenyhetrachlorophthalimidine,④ Otachloro - naphthalene,⑤ 1,2,3,4 - tetrafluoro - benzene, ⑥2,3,4,5 - tetrafluoro - benhydrol etc. therein ： ① with 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 - phenyltertrochlorophthalimidine 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 efficient and lower toxicity. Quinolone drug was synthesis from 2,3,4,5 -Tetrafluombenzoic 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.

关 键 词：2 3 4 5-四氟苯甲酸 喹诺酮 氟喹诺酮 医药中间体 抗生素 

分 类 号：O625.3[理学—有机化学]