(4As-Cis)-1-Cyclopropyl-7-(2,8 Diazabicyclo[4.3.0]Non-8-yl)-6-Fluoro-8-Methoxy-4-Oxo-1,4-Dihydro-3-Quinoline Carboxylic Aid-O3,O4-Bis(Propyloxy-O)Borate.置于盐酸,氨体系中,用 甲醇,水 用作溶剂,化学反应 2.0H,以90%的收率获得莫西沙星 参考文献:Process For The Synthesis Of Moxifloxacin Hydrochloride 标题:Process For The Synthesis Of Moxifloxacin Hydrochloride 摘要:描述了莫西沙星盐酸盐的一种新的多晶形态,以及制备该多晶形态的方法.此外,还描述了莫西沙星盐酸盐形成过程中的新中间体,其化学式为(i)和(II).
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-8680276-B2 优先权日:2009-03-06 标题 :Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine 发明人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO 权利人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO 摘要:The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
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-2025101716-A1 优先权日:2023-11-07 标题:Processes for synthesis of trifunctionalized sulfur(vi) compounds 发明人:LOPCHUK JUSTIN; SHULTZ ZACHARY; ATHAWALE PARESH 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure describes processes for the asymmetric synthesis of trifunctionalized sulfur(VI) containing organic compounds of Formula I and Formula VI, as well as compounds of Formula I and Formula VI prepared by the processes described.
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: Attia TZ, Abbas AM, Nour El-Deen DAM, Omar MA. Zinc (II)-Chelation-Enhanced Spectrofluorimetric Determination of Moxifloxacin: Development, Validation, Application to Eye Drops, and Greenness Assessment. Luminescence. 2026 Apr;41(4):e70483. doi: 10.1002/bio.70483. 2006–. Moxifloxacin. 2026 Apr 15. 27(7):3057. doi: 10.3390/ijms27073057. 5: Bock M, Van Hasselt JGC, Fuursted K, Ihlemann N, Gill S, Christiansen U, Bruun NE, Povlsen JA, Køber L, Høfsten DE, Fosbøl EL, Pries-Heje MM, Thomsen K, Rosenvinge FS, Torp-Pedersen C, Helweg-Larsen J, Tønder N, Iversen K, Bundgaard H, Moser C. Pharmacokinetic and Pharmacodynamic Evaluations of Oral Moxifloxacin for Enterococcus faecalis Endocarditis. Clin Microbiol Infect. 2026 Apr 8:S1198-743X(26)00183-7. doi: 10.1016/j.cmi.2026.04.001. Epub ahead of print. 21(4):e0346333. doi: 10.1371/journal.pone.0346333.
合成参考文献
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