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3-氯-2,4,5-三氟苯甲酸的合成 被引量:1

Synthesis of 3-chloro-2,4,5-trifluorobenzoic acid
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摘要 目的 :合成 3 氯 2 ,4,5 三氟苯甲酸。方法 :以 3 ,4,5 ,6 四氟苯二甲酸为起始原料 ,经酯化、氨化、重氮化和桑德迈耳反应制得 3 氯 2 ,4,5 三氟苯甲酸。结果 :酯化时使用发烟硫酸 ;重氮化和桑德迈耳反应时溶剂由水改为水和二氯乙烷 ,使产率增加 ,质量提高。结论 :该合成路线条件温和 ,操作简单 ,收率提高到 61 .8%。 Objective:To synthesize 3 chloro 2,4,5 trifluorobenzoic acid.Methods:The 3 chloro 2,4,5 trifluorobenzoic acid was prepared by esterification,aminogenesis,diazotisation and Sandmeyer reaction of 3,4,5,6 tetrafluorophthalic acid.Results:In the esterification step,fuming sulfuric acid was used;for increased yield and quality,water was substituted by water and dichloroethane as solvent in the process of diazotisation and Sandmeyer reaction.Conclusion:This synthetic process is mild,convenient,simple and gives good yield to 61.8%. [
机构地区 天津药物研究院
出处 《中国新药杂志》 CAS CSCD 北大核心 2002年第6期468-469,共2页 Chinese Journal of New Drugs
关键词 3-氯-2 4 5-三氟苯甲酸 3 4 5 6-四氟苯二甲酸 合成 chloro 2,4,5 trifluorobenzoic acid 3,4,5,6 tetrafluorophthalic acid synthesis
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  • 1Pillar CM, Zureno GE. Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria [J]. Antimicrob Agents Chemother, 2009, 53 (8) : 3552-3560.
  • 2Teped IME, Hellerw H, Usner DW, et al. Phase III efficacy and safety study of besifloxacin ophthalmic suspension 0.6 % in the treatment of bacterial conjunctivitis [J]. Curr MedRes Opin, 2009, 25 (5) : 1159-1169.
  • 3Blad6-Font A. Facile synthesis of y-, a-, and c-lactams by cyclodehydration of w-amino acids on alumina or silica gel [J]. Tetrahedron Lett, 1980, 21 (25) : 2443-2446.
  • 4Pellegata R, Pinza M, Pifferi G. An improved synthesis of γ-, δ-, and ε-lactams [J]. Synth Commun, 1978, 614-616.
  • 5Boyle WJ, Sifniades S, Peppen JF, et al. Asymmetric transformation of et-amino-e-caprolactam, a lysine precursor [J]. JOrg Chem, 1979, 44 (26) : 4841-4847.
  • 6Stranix BR. HIV protease inhibitors based on amino acid derivatives: US, 6506786 [P]. 2003-01-14.
  • 7Minoru I, Yukiko H, Dai K, et al. Tricyclic pharmacophore- based molecules as novel integrin α, ν, β antagonists. Part III: Synthesis of potent antagonists with ανβ3 dual activity and improved water solubility [J]. Bioorg Med Chem, 2006, 14 (7) : 2131-2150.
  • 8Harms AE. Quinolone carboxylic acids, derivatives thereof, and methods of making and using same: WO, 2008046573 [P]. 2008-04-17.
  • 9Kenichi S, Rumiko S, Atsushi Y, et al. Practical continuous resolution of u-amino-e-caprolaetam by diastereomeric salt formation using a single resolving agent with a solvent switch method [J]. Tetrahedron Asymmetry, 2003, 14: 3713-3718.
  • 10Alexander A, Belyaev EV. A novel synthetic route to N6- methyl-L-lysine and NLmethyl-L-omithine via N3-protected (S)-3-aminolactams [J]. Synthesis, 1991, 5: 417-419.

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