CAS: 145218-19-5; 5-Bromo-2-(Bromomethyl)Pyridine

该化合物是溴化的衍生物,广泛用作有机合成和制药应用的多用途中间体,其主要优点包括:由于存在两个溴替代物,反应性很强,使甲基和的方位能够有选择地发挥作用.该化合物在交叉反应,核生殖替代和作为环环化化合物的建筑块方面特别宝贵.在标准条件和明确界定的再活动特征下,其稳定性成为开发复杂分子结构的研究人员的可靠选择.该产品由于对水和光的敏感性,通常在受控制的条件下处理.

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754131-60-7 168823-76-5 3430-13-5

上下游产品

5-(bromomethyl)-2-methylpyridine 5-bromo-2-methylpyridine (5-bromopyridin-2-yl)methyl methanesulfonate (5-bromopyridin-2-yl)methanol4-(5-bromo-pyridin-2-ylmethoxy)-1-[2-(4-hydroxymethyl-phenyl)-ethyl]-1H-pyridin-2-one 5-bromo-2-(chloromethyl)pyridine N-(diphenylmethylene)-6-(methylsulfonylmethyl)pyridin-3-amine phenyl 6-(methylsulfonylmethyl)pyridin-3-ylcarbamate

合成工艺路线路线简述

    📜(5-Bromopyridin-2-yl)Methyl Methanesulfonate置于lithium Bromide体系中,用 丙酮 用作溶剂,化学反应 1.0H,反应生成5-溴-2-(溴甲基)吡啶
    参考文献:Synthesis And Structure−activity Relationships Of Aza-And Diazabiphenyl Analogues Of The Antitubercular Drug (6S)-2-Nitro-6-{[4-(Trifluoromethoxy)Benzyl]Oxy}-6,7-Dihydro-5H-Imidazo[2,1-B][1,3]Oxazine (Pa-824)
    标题:Synthesis And Structure−activity Relationships Of Aza-And Diazabiphenyl Analogues Of The Antitubercular Drug (6S)-2-Nitro-6-{[4-(Trifluoromethoxy)Benzyl]Oxy}-6,7-Dihydro-5H-Imidazo[2,1-B][1,3]Oxazine (Pa-824)
    摘要:New Heterocyclic Analogues Of The Potent Biphenyl Class Derived From Antitubercular Drug Pa-824 Were Prepared,Aiming To Improve Aqueous Solubility But Maintain High Metabolic Stability And Efficacy. The Strategy Involved Replacement Of One Or Both Phenyl Groups By Pyridine,Pyridazine,Pyrazine,Or Pyrimidine,In Order To Reduce Lipophilicity. For Para-Linked Biaryls,Hydrophilicities (Clogp) Correlated With Measured Solubilities,But Highly Soluble Bipyridine Analogues Displayed Weak Antitubercular Activities. A Terminal Pyridine Or Proximal Heterocycle Allowed Retention Of Potency And Provided Solubility Improvements,Particularly At Low Ph,With Examples From The Latter Classes Displaying The Better In Vivo Efficacies,High Metabolic Stabilities,And Excellent Pharmacokinetics. Five Such Compounds Were >100-Fold Better Than The Parent Drug In A Mouse Model Of Acute Mycobacterium Tuberculosis Infection,And Two Orally Bioavailable Pyridine Analogues (3-4-Fold More Soluble Than The Parent At Low Ph) Were Superior To Antitubercular Drug Opc-67683 In A Chronic Infection Model.
    Doi:10.1021/jm101288T

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    专利信息


    专利号:US-9839642-B2
    优先权日:2014-05-09
    标 题:Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors
    发明人:TANG HAIFENG; YANG SHU-WEI; MANDAL MIHIR; SU JING; LI GUOQING; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; PAN JIANPING; HAGMANN WILLIAM; DING FA-XIANG; XIAO LI; PASTERNAK ALEXANDER; HUANG YUHUA; DONG SHUZHI; YANG DEXI
    权利人:MERCK SHARP & DOHME
    摘要:The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

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