CAS: 82664-20-8; Flurithromycin

该化合物是一种主要用于抗菌特性的大型抗生素,其特征是它能够抑制细菌蛋白合成,与50-S的脊髓膜炎分元素结合,从而有效干扰易感染细菌的生长;该化合物因其针对各种抗乳腺阳性细菌和某些克格鲁阴性细菌的活动而得到特别的注意,使其在治疗呼吸道感染和其他细菌方面有所助益;氟甲色素因其独特的化学结构而有所区别,这种结构包括一个乳胶环和各种功能组,以提高其药理效果和生物利用率;此外,该物质具有一种有利的药理动能特征,可以有效施用剂量疗法;该物质通常通过口服施用,在胃肠道中具有很好的吸收作用;与许多抗生素一样,抗药性发展的潜力令人关切,需要在临床环境中谨慎使用.

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上下游产品

Selectfluor erythromycin

合成工艺路线路线简述

    📜红霉素,N-氟代双苯磺酰胺 以 溶剂黄146,四氢呋喃 作为反应溶剂,化学反应 20.0H,以to Afford Only 0.93 G (7% Yield) Of Crude Flurithromycin的收率获得产物氟红霉素
    参考文献:Preparation Of (8S)-8-Fluoroerythromycins With N-F Fluorinating Agents
    标题:Preparation Of (8S)-8-Fluoroerythromycins With N-F Fluorinating Agents
    摘要:(8S)-8-氟红霉素是通过将8,9-去水红霉素6,9-半缩醛或其n-氧化物与羧酸和n-F氟化试剂反应制备而成.去水起始材料可以在红霉素或其n-氧化衍生物中原位制备. (8S)-8-氟红霉素产品是有用的抗菌剂.

    海关参考信息

    专利信息


    专利号:WO-2015014261-A1
    优先权日:2013-07-30
    标 题:Macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof
    发明人:SHEN SHUNYI; CHEN DAIJIE; GE HAN; ZHANG ZHIHONG; REN YANSONG; LI ZHONGLEI; FAN QIANYONG; ZHANG YUN; XU YIJUN; LI DAN; LI JIAN
    权利人:SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY; CHINA STATE INST PHARM IND
    摘要:The present invention discloses a macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof. The present invention provides a method for preparing a macrolide compound 1, a macrolide compound 1', or a salt thereof; also provided are a macrolide compound 2, macrolide compound 2', or salt thereof, a pharmaceutical composition containing said compound or salt, and the application thereof in the preparation of a pharmaceutical for inhibiting methicillin-resistant Staphylococcus aureus. When one or more of the macrolide compound 2, the macrolide compound 2', the macrolide compound 2 salt, and the macrolide compound 2' salt of the present invention is used together with a β-lactam antibiotic, the inhibiting effect of the β-lactam antibiotic on methicillin-resistant Staphylococcus aureus is significantly increased. This is a new class of potentiator having a good potentiating effect in vitro, alleviating methicillin-resistant Staphylococcus aureus resistance to β-lactam antibiotics, and having good prospects for market development.

    专利号:US-4673736-A
    优先权日:1983-07-18
    标题:Process for the preparation of (8S)-8-fluoroerythromycins
    发明人:TOSCANO LUCIANO
    权利人:PIERREL SPA
    摘要:For the synthesis of (8S)-8-fluoroerythromycins the corresponding 8,9-anhydroerythromycins 6,9-hemiketal are directly fluorinated with perchloryl fluoride.

    专利号:US-10472663-B2
    优先权日:2015-01-21
    标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
    发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
    权利人:ABM TECH LLC
    摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

    专利号:JP-S58109496-A
    优先权日:1981-11-27
    标题:Chemical method of synthesis of macrolide antibiotics

    专利号:KR-840002413-A
    优先权日:1981-11-27
    标题 :Synthesis of macromolecular antibiotics

    专利号:KR-880001566-B1
    优先权日:1981-11-27
    标题:Chemical synthesis of macrolide antibiotics

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    主要参考文献


    1: Fanos V, Mormile R, Benini D, Vecchini S, Cuzzolin L. Flurithromycin-induced acute interstitial nephritis. Pediatr Infect Dis J. 2000 Apr;19(4):366-7. doi: 10.1097/00006454-200004000-00027. 30(3):261-72. doi: 10.1093/jac/30.3.261. 16(2):151-5. doi: 10.1179/joc.2004.16.2.151. 13(3):255-9. doi: 10.1179/joc.2001.13.3.255. 17(2):151-4. doi: 10.1016/s0924-8579(00)00315-0. 32(12):1875-8. doi: 10.1128/AAC.32.12.1875.
    7: Lepore AM, Bonardi G, Maggi GC. Influence of food on the absorption of flurithromycin in man. Int J Clin Pharmacol Res. 1988;8(4):253-7. 5(3):177-84. 812(1-2):255-86. doi: 10.1016/s0021-9673(98)00276-3.
    30:57-88. doi: 10.1016/s0079-6468(08)70375-8.

    合成参考文献


    摘要:Drugs of the Future., 12(214), 1987
    参考文献:10.2165/00003088-199223020-00004
    摘要:Periti P, Mazzei T, Mini E, Novelli A. Pharmacokinetic drug interactions of macrolides. Clin Pharmacokinet. 1992 Aug;23(2):106–31. doi: 10.2165/00003088-199223020-00004.
    摘要:Cuzzolin L, Fracasso ME, Leone R, Benoni G. Effects of erythromycin, flurithromycin and teicoplanin on rat microflora. J Chemother. 1989 Jul;1(4 Suppl):196–7.
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