📜溴乙烷,6,7-Methylenedioxy-4(1H)-Oxo-Cinnolin-3-Carboxylic Acid Ethylester,甲基三辛基氯化铵置于sodium Hydroxide,Potassium Carbonate体系中,用 水,甲苯 用作溶剂,化学反应生成西诺沙星 参考文献:Method For The Production Of 标题:Method For The Production Of 摘要:本发明公开了一种制备1-烷基-4(1H)-氧代-香豆素-3-羧酸的方法.将甲基草酸双烷基酯-3,4-亚甲基二氧基-苯基肼用1至1.5摩尔碱皂化成相应的单烷基酯,然后在羧酸酐存在下,通过friedel-Crafts催化剂环化成6,7-亚甲基二氧基-4(1H)-氧代-香豆素-3-羧酸烷基酯,随后在适当的溶剂中,在碱的存在下,用c.Sub.1-C.Sub.4烷基卤化物烷基化,然后皂化酯.通过短暂加热和从碱性溶液中沉淀除去少量的2-位置烷基化副产物,留下纯的1-烷基产物.该产品可用于治疗尿路感染.
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:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
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:WO-2012149093-A1 优先权日:2011-04-26 标 题 :2-guanidino-4-oxo-imidazoline derivatives as antimalarial agents, synthesis and methods of use thereof 发明人:LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 权利人:US OF AMERICA AS REPRESENTED BY THE SECRETARY OF ARMY; LIN AI J; LIU XIANJUN; KOZAR MICHAEL P; O'NEIL MICHAEL T 摘要:The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
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.
1: Quercia O, Rafanelli S, Emiliani F, Stefanini GF. Anaphylactic reaction to cinoxacin: report of one case associated with inferior acute myocardial infarction. Eur Ann Allergy Clin Immunol. 2003 Feb;35(2):61-3. Italian. Italian. Italian. Japanese. Italian. Italian. Italian. 19: Brogard JM, Comte F, Lavillaureix J. Comparative pharmacokinetic profiles of cinoxacin and pipemidic acid in humans. Eur J Drug Metab Pharmacokinet. 1983 Jul-Sep;8(3):251-9.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198 摘要: 摘要:Li, J. J., Science of Synthesis: Knowledge Updates, (2025) 2.