2-Phenylimidazo[1,2-a]pyridine-8-carboxamide | 353456-64-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-Phenylimidazo[1,2-a]pyridine-8-carboxamide
• CAS: 353456-64-1
• 化学式: C₁₄H₁₁N₃O
• 分子量: 237.261
• InChiKey: ZSDDHVOOAAACCZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  60.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-Phenylimidazo[1,2-a]pyridine-8-carboxamide 、 t-butyldimethylsilane 在 二叔丁基过氧化物 、 zinc trifluoromethanesulfonate 作用下， 反应 36.0h， 以60%的产率得到5-(tert-butyldimethylsilyl)-2-phenylimidazo[1,2-a]pyridine-8-carboxamide
  参考文献：
  名称：

  Selective C-5 Oxidative Radical Silylation of Imidazopyridines Promoted by Lewis Acid

  摘要：

  An oxidative cross dehydrogenative coupling of imidazopyridines with silanes was developed using di-tert-butyl peroxide as the oxidant. The coordination effect of Lewis acid was the dominant factor controlling the regioselective addition of silyl radical to imidazopyridines, and the corresponding C-5 silylated imidazo[1,2-a]pyridines were obtained in moderate to high yields with a broad substrate scope.

  DOI：

  10.1021/acs.orglett.0c02131
• 作为产物：
  描述：

  、 1-羟基苯并三唑 、 氨 、 1-(3-二甲基氨基丙基)-3-乙基碳二亚胺 、 二氯甲烷 、 N,N-二甲基甲酰胺 在 碳酸氢钠 、 乙酸乙酯 、 水 作用下， 以 1,4-二氧六环 为溶剂， 反应 16.0h， 以0.25 g of product was obtained的产率得到2-Phenylimidazo[1,2-a]pyridine-8-carboxamide
  参考文献：
  名称：

  Heterocyclic compounds and their use as parp inhibitors

  摘要：

  本发明涉及式（I）的化合物，其中：A1或A2表示CONH2，而另一个基团A2或A1表示氢，氯，氟，溴，碘，C1-C6烷基，OH，硝基，CF3，CN，NR11R12，NH-CO-R13，O-C1-C4烷基; X1可以表示N和C-R2; X2，独立于X1，可以表示N和C-R2; R2可以表示氢，C1-C6烷基，C1-C4烷基苯基，苯基; B可以表示最多具有15个碳原子的不饱和，饱和或部分不饱和的单环，双环或三环环，最多具有14个碳原子和0至5个氮原子，0至2个氧原子或0至2个硫原子的不饱和，饱和或部分不饱和的单环，双环或三环环，它们仍然可以被R4取代，最多3个相同或不同的基团R5，以及; R1，R4，R5，R11-R13具有权利要求1中所述的含义。本发明还涉及所述化合物的互变异构体形式，可能的对映异构体和顺反异构体形式，它们的前药及其作为PARP抑制剂的用途。

  公开号：

  US20030134843A1

文献信息

• Electrochemical C3-methylthiolation of imidazopyridines with dimethyl sulfoxide
  作者：Zhaoyue Feng、Yingsibing Fan、Congcong Qiang、Ping Liu、Peipei Sun

  DOI：10.1039/d4gc00314d

  日期：——

  An efficient electrochemical methylthiolation reaction of imidazo[1,2-a]pyridines was achieved. The method used DMSO as both the methylthiolating reagent and solvent and KI as both the hydrogen atom transfer reagent and supporting electrolyte. The reaction was performed under transition metal- and chemical oxidant-free conditions. For various substituted 2-arylimidazo[1,2-a]pyridines, C-3 methylthiolation

  实现了咪唑并[1,2- a ]吡啶的高效电化学甲硫基化反应。该方法使用DMSO作为甲硫基化试剂和溶剂，KI作为氢原子转移试剂和支持电解质。该反应在无过渡金属和化学氧化剂的条件下进行。对于各种取代的2-芳基咪唑并[1,2- a ]吡啶，以良好的产率区域选择性地获得了C-3甲基硫基化产物。
• Pharmaceutical Compositions and Method for Treating, Reducing, Ameliorating, Alleviating, or Preventing Dry Eye
  申请人：Zhang Jinzhong

  公开号：US20080305994A1

  公开（公告）日：2008-12-11

  A composition for treating, reducing, ameliorating, alleviating, or preventing a dry eye condition or an opthalmologic disorder that has an etiology in inflammation comprises an inhibitor of activity of poly(ADP-ribose) polymerase (“PARP”). The composition can also include a modulator of pro-inflammatory gene expression.
• USE OF DIANHYDROGALACTITOL OR DERIVATIVES OR ANALOGS THEREOF FOR TREATMENT OF PEDIATRIC CENTRAL NERVOUS SYSTEM MALIGNANCIES
  申请人：DelMar Pharmaceuticals, Inc.

  公开号：US20180071244A1

  公开（公告）日：2018-03-15

  The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of malignancies of the central nervous system in pediatric patients, including glioblastoma multiforme (GBM) high grade glioma, and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N 7 methylation and that can induce double-stranded breaks in DNA. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide, cisplatin, and tyrosine kinase inhibitors; the drug acts independently of the MGMT repair mechanism. Dianhydrogalactitol can be used together with other anti-neoplastic agents (e.g. cisplatin) and can possess additive or super-additive effects.
• USE OF DIANHYDROGALACTITOL AND DERIVATIVES THEREOF IN THE TREATMENT OF GLIOBLASTOMA, LUNG CANCER, AND OVARIAN CANCER
  申请人：Bacha Jeffrey A.

  公开号：US20190091195A1

  公开（公告）日：2019-03-28

  Substituted hexitol derivatives such as dianhydrogalactitol are useful in the treatment of various neoplastic pathologies. Said pathologies include glioblastoma multiforme, non-small-cell lung carcinoma (NSCLC), ovarian cancer, and leptomeningeal carcinomatosis. The anti-neoplastic activity of dianhydrogalactitol is demonstrated to be due to its activity as an alkylating agent that creates N 7 methylation and inter-strand DNA crosslinks. The hexitol derivatives may be used alone or in combination with other anti-neoplastic agents.
• US7041675B2
  申请人：——

  公开号：US7041675B2

  公开（公告）日：2006-05-09