CAS: 64951-10-6; Imidazo[1,2-A]Pyrimidine-2-Carboxylic Acid

该化合物是一种杂交循环化合物,其特点是一个有碳酸分泌功能组的有引信的imidazole和pymidine环系统的环形体,这种结构在药用化学和药物研究中具有多种用途,特别是作为设计生物活性分子的脚架.其硬性双环框架加强了目标互动的结合和选择性,使其对开发酶抑制剂或受体调节器很有价值. 箱酸混合物允许进一步衍生,促进氨酸酯,酯或其他衍生物的合成. 化合物的稳定性和合成可获取性支持其在高通量筛选和铅优化中的效用. 它通常用于针对炎症,肿瘤或CNS病症的潜在治疗综合.

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64951-06-0 143982-40-5 907945-69-1

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CAS号109-12-6 2-氨基嘧啶 | CAS号1113-59-3 3-溴丙酮酸

合成工艺路线路线简述

    📜1,3,5-三嗪-2,4,6-三胺,N,N'''-1,2-乙二基二[n-[3-[[4,6-二[丁基(2,2,6,6-四甲基-4-哌啶基)氨基]-1,3,5-三嗪-2-基]氨基]丙基]-N,N''-二丁基-N,N''-二(2,2,6,6-四甲基-4-哌啶基)-,3-溴丙酮酸置于对甲苯磺酸体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,125.0 °C,400.01 Kpa 条件下,反应 0.17H,以60%的收率获得产物咪唑[1,2-A]嘧啶-2-羧酸
    参考文献:高功能化咪唑并[1,2-A]杂环的全自动连续流动合成
    标题:高功能化咪唑并[1,2-A]杂环的全自动连续流动合成
    摘要:第一个直接从 2-氨基吡啶和溴丙酮酸连续流动合成咪唑并[1,2-A]吡啶-2-羧酸的方法已经开发出来,这代表了相对于相应烧瓶内方法的显着进步.该工艺适用于咪唑并[1,2-A]吡啶-2-甲酰胺(包括mur连接酶抑制剂)的多步合成,使用两个微反应器,多步连续流动工艺,无需分离中间体.
    DOI:10.1021/ol902433A

    海关参考信息

    专利信息


    专利号:US-8841306-B2
    优先权日:2008-11-20
    标 题:Antimicrobials
    发明人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; KANWAR SANDEEP; MAGADI SITARAM KUMAR; SHARMA SUDHIR KUMAR
    权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; KANWAR SANDEEP; MAGADI SITARAM KUMAR; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
    摘要:The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella , acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

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    合成参考文献


    参考文献:10.1186/s13065-015-0121-4
    摘要:Kethireddy S, Eppakayala L, Maringanti TC. Synthesis and antibacterial activity of novel 5,6,7,8-tetrahydroimidazo[1,2-a]pyrimidine-2-carbohydrazide derivatives. Chemistry Central Journal. 2015 Sep 24;9(1). doi: 10.1186/s13065-015-0121-4.
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