左旋氧氟沙星羧酸 以 N-甲基哌嗪,正庚烷 用作溶剂,化学反应生成左氧氟沙星 参考文献:Preparation Of Levofloxacin And Forms Thereof 标题:Preparation Of Levofloxacin And Forms Thereof 摘要:左氧氟沙星是通过将(S)-(−)-9,10-二氟-3-甲基-7-氧代-2,3-二氢-7H-吡啶[1,2,3-De][1,4]苯并噁唑-6-羧酸与n-甲基哌嗪在极性溶剂或无溶剂混合物中反应制备而成.进一步处理左氧氟沙星可产生新的左氧氟沙星形式,包括半水合物和a,B,C,F,G和h形式.
专利号:US-12383499-B2 优先权日:2018-01-01 标题:Scale up synthesis of silicasome nanocarriers 发明人:NEL ANDRE E; MENG HUAN; LIU XIANGSHENG 权利人:UNIV CALIFORNIA 摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).
专利号:US-5521310-A 优先权日:1992-10-07 标 题 :Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives 发明人:CARRETERO GONZALVEZ JUAN-CARLO; VICIOSO SANCHEZ MERCEDES; GARCIA RUANO JOSE-LUIS 权利人:ETILO DERIVADOS 摘要:A process to obtain benzoxazines useful for the synthesis of Ofloxazine, Levofloxazine and derivatives. The benzoxacines (I) where Xb is an halogen and R 1 is H, alkyl or alkenyl of up to 6 atoms of C or aryl, can be obtained by means of cycling a compound of formula (II) through the reaction with triphenylphosphine and ethyl azodicarboxilate. The compounds of formula (II) can be obtained through the reaction of a compound (III) with an adequate epoxide. Through the use of the adequate chiral epoxide it is possible to obtain the enantiomerically desired intermediate and, therefore and selectively, it is possible to obtain the desired final product with the adequate enantiomeric form without the need to carry out a resolution stage. n The Compounds (I) are useful and key intermediates for the synthesis of the antimicrobials Oflixazine and Levofloxazine. ##STR1##
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:US-11059835-B2 优先权日:2014-08-15 标 题 :Synthesis of cephalosporin compounds 发明人:WALLER DAVID; GAZDA GREGORY; MINDEN ZACHARY; BARTON LISA; LEIGH CLIFTON 权利人:MERCK SHARP & DOHME 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction.
专利号:US-2011087037-A1 优先权日:2007-10-31 标题:Synthesis of ring b abeo-sterols as novel inhibitors of mycobacterium tuberculosis 发明人:RODRIGUEZ-PIERLUISSI ABIMAEL D; WEI XIAOMEI 权利人:INTELLECTUAL PROPERTY AND TECHNOLOGY VIC OFF OF 摘要:Novel 3β-hydroxy-Δ 5 -steroid analogs possessing a contracted cyclopentane B-ring provide good inhibitory activity against Mycobacterium tuberculosis . The 5(6→7)abeo-sterol nucleus present in compounds of the invention represents a novel scaffold for the development of new antitubercular agents.
1: Charfi O, Lakhoua G, Sahnoun R, Badri T, Daghfous R, El Aidli S, Kastalli S, Zaïem A. DRESS Syndrome Following Levofloxacin Exposure With Positive Patch-test. Therapie. 2015 Nov-Dec;70(6):547-9. doi: 10.2515/therapie/2015046. Epub 2015 Aug 3. Review. doi: 10.1517/14740338.2015.989210. Epub 2014 Dec 10. Review. 3: Stockmann C, Hillyard B, Ampofo K, Spigarelli MG, Sherwin CM. Levofloxacin inhalation solution for the treatment of chronic Pseudomonas aeruginosa infection among patients with cystic fibrosis. Expert Rev Respir Med. 2015 Feb;9(1):13-22. doi: 10.1586/17476348.2015.986469. Epub 2014 Nov 24. Review. Review. Polish. doi: 10.1055/s-0034-1375964. Epub 2014 May 31. Review. doi: 10.1002/pds.3581. Epub 2014 Feb 21. Review. doi: 10.3109/00365521.2014.887765. Epub 2014 Mar 11. Review. doi: 10.1177/1753465813508445. Epub 2013 Dec 10. Review. doi: 10.2147/TCRM.S59079. eCollection 2014. Review. 10: Rafat C, Debrix I, Hertig A. Levofloxacin for the treatment of pyelonephritis. Expert Opin Pharmacother. 2013 Jun;14(9):1241-53. doi: 10.1517/14656566.2013.792805. Epub 2013 Apr 24. Review. doi: 10.3748/wjg.v18.i40.5669. Review.
合成参考文献
参考文献:10.1046/j.1365-2710.2002.00396.x 摘要:Chow AT, Chen A, Lattime H, Morgan N, Wong F, Fowler C, Williams RR. Penetration of levofloxacin into skin tissue after oral administration of multiple 750 mg once-daily doses. J Clin Pharm Ther. 2002 Apr;27(2):143–50. doi: 10.1046/j.1365-2710.2002.00396.x.