9-Fluoro-5-Methyl-1-Oxo-6,7-Dihydro-1H,5H-Pyrido[3,2,1-Ij]Quinoline-2-Carboxylic Acid Ethyl Ester置于水体系中,化学反应 3.0H,以70.8%的收率获得产物氟甲喹 参考文献:Synthesis,Absolute Configuration And Intermediates Of 9-Fluoro-6,7-Dihydro-5-Methyl-1-Oxo-1H,5H-Benzo[i,J]Quinolizine-2-Carboxylic Acid (Flumequine) 标题:Synthesis,Absolute Configuration And Intermediates Of 9-Fluoro-6,7-Dihydro-5-Methyl-1-Oxo-1H,5H-Benzo[i,J]Quinolizine-2-Carboxylic Acid (Flumequine) 摘要:The Antibacterial Agent 9-Fluoro-6,7-Dihydro-5-Methyl-1-Oxo-1H,5H-Benzo[ij]Quinolizine-2-Carboxylic Acid (Flumequine) Was Synthesized In Optically Active Form From 6-Fluoro-2-Methyl-1,2,3,4-Tetrahydroquinoline (Fthq). Racemic Fthq Was Resolved With The Enantiomers Of 3-Bromocamphor-8-Sulfonic Acid. The Configurations Were Established By X-Ray Structures Of The Two Diastereoisomeric Salts. Enantiomeric Excesses Were Determined By H-1 NMR Analysis. (C) 1999 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0957-4166(99)00071-3
专利号:US-2021107859-A1 优先权日:2018-04-06 标题 :A process for the synthesis of carbon labeled organic compounds 发明人:AUDISIO DAVIDE; CANTAT THIBAULT; DESTRO GIANLUCA 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A process for the synthesis of a carbon labeled organic compound containing a carbon labeled carboxyl group is described. A method of using carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; a process for manufacturing labeled pharmaceuticals and agrochemicals comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; and a process for producing tracers comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure are also described.
专利号:US-10768157-B2 优先权日:2015-10-20 标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples 发明人:KABIR ABUZAR; FURTON KENNETH G 权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.
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.
专利号:US-9693999-B2 优先权日:2011-01-26 标题:Small molecule RNase inhibitors and methods of use 发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE 权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education 摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:EP-0310849-B1 优先权日:1987-10-05 标题:Process for the synthesis of a benzo [ij] quinolizine-2-carboxylic acid derivative 摘要:Process for preparing 6,7-dihydro-9-fluoro-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carbo xylic acid (flumequine, I) wherein 6-fluoro-2-methyl-1,2,3,4-tetrahydroquinoline (II) is reacted in the presence of a catalyst with an alkyl ortho-formate (IX), wherein R3 represents a C1-C4 alkyl, and with a 2,2-disubstituted 1,3-dioxan-4,6-dione, wherein each R1 and R2, which can be the same or different, represents a hydrogen atom, a branched- or straight-chain C1-C6 alkyl or phenyl, or R1 and R2 together represent a polymethylene group -(CH2)n-, n= 4 or 5, so as to form a 2,2-disubstituted 5- [1-(6-fluoro-2-methyl-1,2,3,4-tetrahydroquinolyl)] methylene-1,3-dioxan -4,6-dione of formula (VII): and then said compound of formula (VII) is reacted in the presence of polyphosphoric acid and ethyl polyphosphate, whereby the desired compound (I) is directly obtained and isolated according to conventional methods.
1: Kamagate M, Assadi AA, Kone T, Giraudet S, Coulibaly L, Hanna K. Use of laterite as a sustainable catalyst for removal of fluoroquinolone antibiotics from contaminated water. Chemosphere. 2017 Dec 26;195:847-853. doi: 10.1016/j.chemosphere.2017.12.165. [Epub ahead of print] doi: 10.1016/j.foodchem.2017.11.094. Epub 2017 Nov 26. doi: 10.1016/j.jhazmat.2017.12.011. [Epub ahead of print] doi: 10.1016/j.scitotenv.2017.11.244. [Epub ahead of print] doi: 10.1155/2017/3259073. Epub 2017 Oct 23. 7: Jansomboon W, Boontanon SK, Boontanon N, Polprasert C. Determination and health risk assessment of enrofloxacin, flumequine and sulfamethoxazole in imported Pangasius catfish products in Thailand. J Environ Sci Health B. 2017 Nov 27:1-8. doi: 10.1080/03601234.2017.1388655. [Epub ahead of print] doi: 10.1016/j.foodchem.2017.07.072. Epub 2017 Jul 17. doi: 10.1016/j.micpath.2017.09.020. Epub 2017 Sep 18. doi: 10.14202/vetworld.2017.830-835. Epub 2017 Jul 28.
合成参考文献
参考文献:10.1080/19440049.2011.587028 摘要:Takeda N, Gotoh M, Matsuoka T. Rapid screening method for quinolone residues in livestock and fishery products using immobilised metal chelate affinity chromatographic clean-up and liquid chromatography-fluorescence detection. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2011 Sep;28(9):1168–74. doi: 10.1080/19440049.2011.587028.