莫西沙星置于盐酸体系中,用 甲醇 用作溶剂,化学反应生成盐酸莫西沙星 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-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-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-8198451-B2 优先权日:2006-11-13 标题 :Process for the synthesis of moxifloxacin hydrochloride 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; PATHI SRINIVAS LAXMINARAYAN; PUPPALA RAVIKUMAR; GANGRADE MANISH; KANATHALA SHASHIREKHA 权利人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; PATHI SRINIVAS LAXMINARAYAN; PUPPALA RAVIKUMAR; GANGRADE MANISH; KANATHALA SHASHIREKHA; CIPLA LTD 摘要:A new polymorph of moxifloxacin hydrochloride is described, together with a method for making the polymorph. In addition, new intermediates in the formation of moxifloxacin hydrochloride are described, having formulas (1) and (II):
专利号:WO-2012131629-A1 优先权日:2011-03-31 标题 :A process for preparation of intermediate of moxifloxacin 发明人:WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY 权利人:PIRAMAL HEALTHCARE LTD; WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY 摘要:The present invention provides a process for the preparation of racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I, a key intermediate in the synthesis of moxifloxacin or its pharmaceutically acceptable salts. The process comprises reaction of racemic or chiral tetrahydro-6-(phenylmethyl)-1H- pyrrolo[3,4-b]pyridine-5,7(6H)-dione of formula II with a reducing agent, which is a mixture of two agents, that is mixture of dimethyl sulphate and sodium borohydride or aluminum chloride and sodium borohydride used in a molar ratio ranging from 1:1 to 1: 4, in the presence of a polar solvent at a temperature ranging from 15°C to 45°C 10 to obtain racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I having purity ≥ 96%.
专利号:WO-2009056955-A1 优先权日:2007-10-30 标题 :Amine-bearing phospholipids (abps), their synthesis and use 发明人:ZUMBUEHL ANDREAS 权利人:UNIV BASEL; ZUMBUEHL ANDREAS 摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.
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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