CAS: 151096-09-2; 1-Cyclopropyl-6-Fluoro-7-((4As,7As)-Hexahydro-1H-Pyrrolo[3,4-B]Pyridin-6(2H)-yl)-8-Methoxy-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是一种广泛频谱的氟己酮抗生素,其抗药性强,能防止克格朗阳性,克格朗阴性和非典型细菌病原体,其行动机制包括抑制细菌DNA gyras 和TOpo异构体ase IV,干扰DNA复制和转录;Moxifxoxacin表现出良好的生物利用率,组织渗透和长期的半衰期,允许一次剂量;对呼吸道感染特别有效,包括社区传染的肺炎和急性细菌性脊髓炎,以及皮肤和腹部内感染;该化合物由于其双重目标抑制,其抗药性与早先的氟己酮相比,表现低;口服和静脉配方的稳定性提高了临床效用;已知超敏或QT风险延长的病人,其体内氟化辛酸酯是反毒的.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

CAS号112811-72-0 1-环丙基-6,7-二氟-1,... | CAS号151213-40-0 (S,S)-2,8-二氮杂双环... | CAS号186826-86-8 盐酸莫西沙星 | CAS号1028205-71-1 (4aS,7aS)-tert-... | CAS号112811-70-8 (Z)-3-(环丙基氨基)-2... | CAS号186826-86-8 盐酸莫西沙星

合成工艺路线路线简述

  • 合成目标产物 Moxifloxacin 主要起始原料 1-Cyclopropyl-6,7-Difluoro-1,4-Dihydro-8-Methoxy-4-Oxo-3-Quinolinecarboxylic Acid And Cis-Octahydropyrrolo[3,4-B]Pyridine
  • (文献来源)合成步骤主要原料 1-Cyclopropyl-6,7-Difluoro-1,4-Dihydro-8-Methoxy-4-Oxo-3-Quinolinecarboxylic Acid 和 Cis-Octahydropyrrolo[3,4-B]Pyridine
(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).

海关参考信息

专利信息


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.
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主要参考文献


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


参考文献:10.1001/archophthalmol.2011.168
摘要:Davies BW, Panday V, Caldwell M, Scribbick F, Reilly CD. Effect of topical immunomodulatory interleukin 1 receptor antagonist therapy on corneal healing in New Zealand white rabbits (Oryctolagus cunniculus) after photorefractive keratectomy. Arch Ophthalmol. 2011 Jul;129(7):909–13. doi: 10.1001/archophthalmol.2011.168.
摘要:Roberts S, Heffernan H, Al Anbuky N, Pope C, Paviour S, Camp T, Swager T. Molecular epidemiology and susceptibility profiles of Clostridium difficile in New Zealand, 2009. N Z Med J. 2011 Apr 15;124(1332):45–51.
参考文献:10.1007/s10096-011-1326-7
摘要:Tatano Y, Sano C, Yasumoto K, Shimizu T, Sato K, Nishimori K, Matsumoto T, Yano S, Takeyama H, Tomioka H. Correlation between variable-number tandem-repeat-based genotypes and drug susceptibility in Mycobacterium avium isolates. European Journal of Clinical Microbiology & Infectious Diseases. 2011 Jul 12;31(4):445–54. doi: 10.1007/s10096-011-1326-7.
参考文献:10.3201/eid/1706.101037|10.3201/eid1706.101037
摘要:Aguado JM, San-Juan R, Lalueza A, Sanz F, Rodríguez-Otero J, Gómez-Gonzalez C, Chaves F. High Vancomycin MIC and Complicated Methicillin-SusceptibleStaphylococcus aureusBacteremia. Emerg. Infect. Dis. 2011 Jun;17(6):1099–102. doi: 10.3201/eid/1706.101037.
参考文献:10.1128/mbio.00108-11
摘要:Drusano GL, Sgambati N, Eichas A, Brown D, Kulawy R, Louie A. Effect of administration of moxifloxacin plus rifampin against Mycobacterium tuberculosis for 7 of 7 days versus 5 of 7 days in an in vitro pharmacodynamic system. mBio. 2011;2(4):e00108–11.
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