专利号:WO-2015198349-A1 优先权日:2014-06-25 标 题 :A one pot synthesis of 3-substituted quinoline carboxylates and its derivatives 发明人:GADAKH SUNITA KHANDERAO; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a one pot, simple, cost effective and industrially feasible catalytic synthesis of quinolines or substituted quinolines from anilines with yield >80% yield. The present invention also discloses a process for the synthesis of oxolinic acid using quinolines with yield > 45%.
专利号:US-5475116-A 优先权日:1994-04-29 标题:Aza bicyclo[3,1,0]hexane intermediates useful in the synthesis of quinolones 发明人:BRIGHTY KATHERINE E; BRAISH TAMIM F 权利人:PFIZER 摘要:This invention relates to certain azabicyclo hexane intermediates and processes for making and using the azabicyclo hexane intermediates. The intermediates are useful in the synthesis of quinolone antibacterial agents.
专利号:US-11332444-B2 优先权日:2018-04-25 标题:Method for the hydrolysis of quinolonecarboxylic esters 发明人:FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE 权利人:BAYER ANIMAL HEALTH GMBH 摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.
专利号:US-12252473-B2 优先权日:2022-04-18 标 题:Preparation methods of quinolone compounds and intermediates thereof 发明人:LEI JIE; CHEN ZHONGZHU; XU ZHIGANG; TANG DIANYONG; XU JIAYU; ZHOU HAOYI; XIA DANDAN; LIU YAO; CAO YIHUA; LUO JIE 权利人:UNIV CHONGQING ARTS & SCIENCES 摘要:The present application relates to processes for the preparation of quinolone compounds and intermediates thereof, particularly to processes for the preparation of quinolones and pharmaceutical intermediates of the quinolones. In particular, the present application provides a process for the preparation of a compound of Formula I, and a process for the synthesis of quinolone compounds using the compound of Formula I as an intermediate. The process for the preparation of the compound of Formula I comprises the steps of:reacting a compound of Formula A with R5NH2 and R6Cl in the presence of a base to form the compound of Formula I,
专利号:WO-2025056767-A1 优先权日:2023-09-15 标题 :Process for the preparation of enantiomerically enriched aliphatic amines 发明人:BOU HAMDAN FARHAN; GODINEAU EDOUARD; SMEJKAL TOMAS; DUMEUNIER RAPHAEL; BOUSSEMGHOUNE MOHAMED ABDELOUAHAB; BLUM MATHIAS 权利人:SYNGENTA CROP PROTECTION AG 摘要:The present invention relates to a process for the preparation of enantiomerically enriched cyclobutylamines of formula (I) from α-tertiary cyclobutanones and reacting said enantiomerically enriched cyclobutylamines to enantiomerically enriched cyclobutylamides. Such compounds are useful intermediates in the synthesis of microbiocidal thiazole compounds.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
1: Pathak R, Mallik SK, Patil PK, Shahi N, Kala K, Bhat RAH, Nadella RK, Pandey N, Pandey PK. Assessment of Single-Dose Pharmacokinetics of Oxolinic Acid in Rainbow Trout and Determination of In Vitro Antibacterial Activity Against Pathogenic Bacteria From Diseased Fish. J Vet Pharmacol Ther. 2024 Aug 9. doi: 10.1111/jvp.13477. Epub ahead of print. 159:29-35. doi: 10.3354/dao03798. 40(26):13596-13602. doi: 10.1021/acs.langmuir.4c01141. Epub 2024 Jun 18. 63(6):773-818. doi: 10.1007/s40262-024-01377-0. Epub 2024 May 28. 5: Aissaoui Y, Jiménez-Skrzypek G, González-Sálamo J, Trabelsi-Ayadi M, Ghorbel- Abid I, Hernández-Borges J. Determination of Multiclass Antibiotics in Fish Muscle Using a QuEChERS-UHPLC-MS/MS Method. Foods. 2024 Apr 1;13(7):1081. doi: 10.3390/foods13071081.
合成参考文献
摘要:The Chemical Society. Foreign Compound Metabolism in Mammals. Volume 1: A Review of the Literature Published Between 1960 and 1969. London: The Chemical Society, 1970., p. 206 摘要:The Merck Index. 9th ed. Rahway, New Jersey: Merck & Co., Inc., 1976., p. 899 摘要: 参考文献:10.1007/bf01953757 摘要:Bertolini A, Castelli M, Genedani S, Garuti M. Trimethoprim enhances the antibacterial activity of nalidixic and oxolinic acids and delays the emergence of resistance. Cellular and Molecular Life Sciences. 1980 Feb;36(2):243–4. doi: 10.1007/bf01953757. 参考文献:10.1007/bf01953758 摘要:Whitehouse RW, Lendon RG, Lendon M. Renal polycystosis in the rat induced by prednisolone tertiary butyl acetate. Cellular and Molecular Life Sciences. 1980 Feb;36(2):244–5. doi: 10.1007/bf01953758.