CAS: 37517-28-5; Amikacin

该化合物是一种主要用于治疗格外阴性细菌造成严重感染的抗生素,特别是在其他抗生素无效的情况下,主要用于治疗克丁酸细菌引起的严重感染;它源自卡纳米素,并展示了各种病原体,包括Pseudomonas aeruginosa和某些菌株的麦基菌肺结核;它通过抑制细菌蛋白合成,导致细胞死亡而进行氨基辛;它通常通过注射进行,因为它从肠胃道吸收的不多;该物质的特点是其毒性相对较低,尽管它仍然可造成肾脏毒性和毒性,但在治疗期间必须仔细监测肾脏功能和药物水平;它通常保留给严重感染者或有抗其他抗生素者;它化学结构包括一个氨基安基安基化合物,有助于其行动机制及药性特性;同所有抗生素一样,适当使用对于防止抗药性的发展至关重要.

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CAS号39831-55-5 硫酸阿米卡星

合成工艺路线路线简述

  • 合成目标产物 Amikacin 主要起始原料 Amikacin Disulfate
  • (文献来源)合成步骤主要原料 Amikacin Disulfate
在 氨,Potassium Carbonate体系中,用 丙酮 用作溶剂,化学反应生成阿米卡星
参考文献:一种硫酸阿米卡星化合物
标题:一种硫酸阿米卡星化合物
摘要:本发明公开了一种硫酸阿米卡星化合物,该化合物用粉末x射线衍射测定法测定,以2θ+/-0.2°衍射角表示在6.3°,13.0°,14.3°,17.2°,18.2°,20.0°,22.7°,23.7°,25.9°,27.5°,29.2°处显示出特征衍射峰.本发明制备的硫酸阿米卡星化合物具有稳定性好,纯度高,杂质少的优点,而且工艺简单,收率高,重复性强,用药安全性和有效性高,大大降低了不良反应的发生率,适合于工业化生产.

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-5763587-A
优先权日:1987-11-27
标题:Process for the synthesis of amikacin
发明人:MANGIA ALBERTO
权利人:GIST BROCADES ITALY SPA
摘要:In the synthesis of amikacin, having the formula: (I) by acylation of a diprotected derivative of kanamycin A with a reactive derivative of L-(-)-4-amino-2-hydroxybutyric acid, the selection of the reaction solvent and of the pH conditions permit the industrial economically and the synthesis yield to be improved.

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-4902790-A
优先权日:1985-10-10
标 题 :Novel process for the synthesis of amikacin
发明人:MANGIA ALBERTO; GIOBBIO VICENZO; ORNATO GIORGIO
权利人:PIERREL SPA
摘要:A novel process for the synthesis of amikacin starting from kanamycin A protected at the positions 3 and 6' is described comprising the reaction of kanamycin A with a salt of a bivalent metal cation selected from zinc, nickel, iron, cobalt, manganese, copper and cadmium in the presence of water as the solvent or co-solvent followed by the in situ reaction of the resulting complex with a reactive derivative of L-amino-2-hydroxy-butyric acid, removal of the metal cation of the protecting groups and purification of the thus obtained raw product. The acylation under these conditions is extremely selective.

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: Rose SJ, Neville ME, Gupta R, Bermudez LE. Delivery of aerosolized liposomal amikacin as a novel approach for the treatment of nontuberculous mycobacteria in an experimental model of pulmonary infection. PLoS One. 2014 Sep 29;9(9):e108703. doi: 10.1371/journal.pone.0108703. eCollection 2014.
2: Zantingh AJ, Schwark WS, Fubini SL, Watts AE. Accumulation of amikacin in synovial fluid after regional limb perfusion of amikacin sulfate alone and in combination with ticarcillin/clavulanate in horses. Vet Surg. 2014 Mar;43(3):282-8. doi: 10.1111/j.1532-950X.2014.12119.x. Epub 2014 Jan 27. doi: 10.1089/jamp.2013.1100.
4: Dudek M, Romanowska J, Wituła T, Trylska J. Interactions of amikacin with the RNA model of the ribosomal A-site: computational, spectroscopic and calorimetric studies. Biochimie. 2014 Jul;102:188-202. doi: 10.1016/j.biochi.2014.03.009. Epub 2014 Apr 24. doi: 10.2146/ajhp130308. doi: 10.1093/jac/dku569. Epub 2015 Jan 27. doi: 10.1007/s00228-014-1766-y. Epub 2014 Oct 21. doi: 10.1016/j.jchromb.2014.01.035. Epub 2014 Jan 30. doi: 10.1007/s00134-014-3308-6. Epub 2014 May 10. Spanish. doi: 10.1128/AAC.01157-15. Epub 2015 Jul 27.

合成参考文献


参考文献:10.1007/s11095-009-0042-9
摘要:Eljarrat-Binstock E, Pe’er J, Domb AJ. New Techniques for Drug Delivery to the Posterior Eye Segment. Pharmaceutical Research. 2010 Feb 13;27(4):530–43. doi: 10.1007/s11095-009-0042-9.
参考文献:10.1177/112067211002000422
摘要:Levy J, Lifshitz T. Keratitis after Implantation of Intrastromal Corneal Ring Segments (Intacs) Aided by Femtosecond Laser for Keratoconus Correction: Case Report and Description of the Literature. European Journal of Ophthalmology. 2010 Jul;20(4):780–4. doi: 10.1177/112067211002000422.
参考文献:10.1086/651024
摘要:Yuan Z, Ledesma KR, Singh R, Hou J, Prince RA, Tam VH. Quantitative assessment of combination antimicrobial therapy against multidrug-resistant bacteria in a murine pneumonia model. J Infect Dis. 2010 Mar 15;201(6):889–97. doi: 10.1086/651024.
参考文献:10.2174/157489110791233540
摘要:Amaral L, Molnar J. Therapy Of XDR TB with thioridazine a drug beyond patent protection but eligible for patent "as new use". Recent Pat Antiinfect Drug Discov. 2010 Jun;5(2):109–14. doi: 10.2174/157489110791233540.
参考文献:10.1186/cc8877
摘要:Augustin P, Kermarrec N, Muller-Serieys C, Lasocki S, Chosidow D, Marmuse JP, Valin N, Desmonts JM, Montravers P. Risk factors for multidrug resistant bacteria and optimization of empirical antibiotic therapy in postoperative peritonitis. Crit Care. 2010;14(1):R20.
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