📜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.
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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合成参考文献
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