2-甲氧基乙氧基甲基氯,红霉素a肟置于sodium Ethanolate体系中,用 丙酮 作为反应溶剂,化学反应 0.42H,反应生成 罗红霉素 参考文献:A Process For The Purification Of Roxithromycin 标题:A Process For The Purification Of Roxithromycin 摘要:一种用于纯化罗红霉素的方法,其中含有高水平杂质-H,包括将不纯的罗红霉素部分溶解和/或悬浮于乙醇,乙腈,芳香溶剂或乙醇和乙腈混合物中的溶剂中,然后结晶,从而获得杂质-H小于0.5%的罗红霉素.本发明还涉及根据上述纯化过程获得的罗红霉素结晶多形体b和c,其杂质-H小于0.5%.
专利信息
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2024197774-A1 优先权日:2021-04-16 标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles 发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO 权利人:UNIV TEXAS 摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.
专利号:WO-2015014261-A1 优先权日:2013-07-30 标 题:Macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof 发明人:SHEN SHUNYI; CHEN DAIJIE; GE HAN; ZHANG ZHIHONG; REN YANSONG; LI ZHONGLEI; FAN QIANYONG; ZHANG YUN; XU YIJUN; LI DAN; LI JIAN 权利人:SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY; CHINA STATE INST PHARM IND 摘要:The present invention discloses a macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof. The present invention provides a method for preparing a macrolide compound 1, a macrolide compound 1', or a salt thereof; also provided are a macrolide compound 2, macrolide compound 2', or salt thereof, a pharmaceutical composition containing said compound or salt, and the application thereof in the preparation of a pharmaceutical for inhibiting methicillin-resistant Staphylococcus aureus. When one or more of the macrolide compound 2, the macrolide compound 2', the macrolide compound 2 salt, and the macrolide compound 2' salt of the present invention is used together with a β-lactam antibiotic, the inhibiting effect of the β-lactam antibiotic on methicillin-resistant Staphylococcus aureus is significantly increased. This is a new class of potentiator having a good potentiating effect in vitro, alleviating methicillin-resistant Staphylococcus aureus resistance to β-lactam antibiotics, and having good prospects for market development.
专利号:WO-2004075874-A1 优先权日:2003-02-28 标题 :Method for treatment and prevention of acute and chronic pseudomonas aeruginosa airway infections with inhalable macrolides 发明人:MENEKSE OKTAY 权利人:ANBICS PATENTS LICENCES AG; MENEKSE OKTAY 摘要:Macrolides, in particular azalides such as azithromycin, are suited for the treatment or prevention of acute or chronic P. aeruginosa infections of the airways by inhalaÂtion. The mechanism of action is the inhibition of the quoÂrum sensing of P. aeruginosa, in particular the impediment of the las and rhl quorum sensing systems synthesis and the impediment of the synthesis of the autoinducers N-[3-oxodoÂ1o decanoyl]-L-homoserine lactone and N-butyrylhomoserine lacÂtone. This allows for inhalation treatments of P. aerugi-nosa infections at non-inhibiting concentrations of the macrolide.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-5912331-A 优先权日:1991-03-15 标题:Process for the preparation of 9-deoxo-9(Z)-hydroxyiminoerythromycin A 发明人:WILKENING ROBERT R 权利人:MERCK & CO INC 摘要:A method is presented for isomerizing the E-isomer of 9-Deoxo-9-hydroximinoerythromycin A to its corresponding Z-isomer. The Z-isomer is useful as an antibiotic and as an intermediate for the synthesis of other macrolide antibiotics.
1: Shafuddin E, Mills GD, Holmes MD, Poole PJ, Mullins PR, Black PN. A double-blind, randomised, placebo-controlled study of roxithromycin and doxycycline combination, roxithromycin alone, or matching placebo for 12 weeks in adults with frequent exacerbations of chronic obstructive pulmonary disease. J Negat Results Biomed. 2015 Sep 7;14:15. doi: 10.1186/s12952-015-0034-8. 2: Choi Y, Koh SJ, Lee HS, Kim JW, Gwan Kim B, Lee KL, Kim JS. Roxithromycin inhibits nuclear factor kappaB signaling and endoplasmic reticulum stress in intestinal epithelial cells and ameliorates experimental colitis in mice. Exp Biol Med (Maywood). 2015 Dec;240(12):1664-71. doi: 10.1177/1535370215591829. Epub 2015 Jun 18. 3: Dai YR, Wu HY, Wu LQ, Xu H, Yin J, Yan SS, Zeng WX. Roxithromycin reduces the viability of cultured airway smooth muscle cells from a rat model of asthma. Eur Rev Med Pharmacol Sci. 2014;18(23):3564-72. doi: 10.1016/j.jiac.2013.07.010. Epub 2013 Dec 11. doi: 10.1097/FTD.0000000000000203. doi: 10.1016/j.ejps.2014.12.019. Epub 2015 Jan 2. doi: 10.1136/bmj.g4930.
合成参考文献
参考文献:10.1097/01.mlg.0000177031.06112.50 摘要:Matsune S, Sun D, Ohori J, Nishimoto K, Fukuiwa T, Ushikai M, Kurono Y. Inhibition of vascular endothelial growth factor by macrolides in cultured fibroblasts from nasal polyps. Laryngoscope. 2005 Nov;115(11):1953–6. doi: 10.1097/01.mlg.0000177031.06112.50. 参考文献:10.1111/j.1365-2885.2011.01322.x 摘要:Wang X, Tao YF, Huang LL, Chen DM, Yin SZ, Ihsan A, Zhou W, Su SJ, Liu ZL, Pan YH, Yuan ZH. Pharmacokinetics of tulathromycin and its metabolite in swine administered with an intravenous bolus injection and a single gavage. J Vet Pharmacol Ther. 2012 Jun;35(3):282–9. doi: 10.1111/j.1365-2885.2011.01322.x. 参考文献:10.2147/opth.s13785 摘要:Utine CA. Update and critical appraisal of the use of topical azithromycin ophthalmic 1% (AzaSite) solution in the treatment of ocular infections. Clin Ophthalmol. 2011;5():801–9.