2-(Iodomethyl)-5-(2-nitroimidazol-1-yl)oxolane-3,4-diol

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(Iodomethyl)-5-(2-nitroimidazol-1-yl)oxolane-3,4-diol
• 化学式: C₈H₁₀IN₃O₅
• 分子量: 355.089
• InChiKey: FWNOUYXMHAJQMU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  113
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-(Iodomethyl)-5-(2-nitroimidazol-1-yl)oxolane-3,4-diol 在 sodium azide 、 四丁基溴化铵 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以70%的产率得到
  参考文献：
  名称：

  [EN] MARKERS, CONJUGATES, COMPOSITIONS AND METHODS FOR HYPOXIA IMAGING, MAPPING, AND THERAPY
  [FR] MARQUEURS, CONJUGUÉS, COMPOSITIONS ET PROCÉDÉS D'IMAGERIE, DE CARTOGRAPHIE ET DE THÉRAPIE DE L'HYPOXIE

  摘要：

  Described herein are markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy. A compound comprising bio-reductively activated (BA) arm, linker arm and a mapping click wherein BA contains one for more of substituted or unsubstituted 2/4/5-substituted nitroimidazoles, or substituted benzotriazene-1,4-dioxides, or substituted 1,2,3/1,2,4-triazoles, or substituted 1,4-benzoquinones, or a combination of two homo-or hetero BA moieties, wherein linker arm contains C1-16 alkane, alkene, alkyne, alicyclic or aromatic linkers with or without hetero atoms as in ethers, amine, esters, acid, amides, 5 and 6 membered sugar sings with the substitution as described above, both monosaccharides and disaccharides, wherein mapping click contains one of substituted or unsubstituted -N3-, CN, SCN, substituted alkynes for click chemistry. Said compound undergoes in situ click reaction after its distribution in cells or tissues to link to a reporting group which may be unchelated or chelated with a metal-radioactive or non-radioactive-, or a radiohalogen for PET/SPECT, or a dye for fluorescent/optical reporting group, thus accomplishing hypoxia imaging.

  公开号：

  WO2019056097A1

文献信息

• COMPOUNDS USEFUL IN IMAGING AND THERAPY
  申请人：Kumar Piyush

  公开号：US20130211066A1

  公开（公告）日：2013-08-15

  Provided in the following specification are precursors or synthons that are useful for the synthesis of various arabinose based chemical and radiochemical derivatives of nitroimidazole-containing azomycin arabinosides, such as radioiodinated 1-#-D-(5-deoxy-5-[I*]-iodoarabinofuranosyl)-2-nitroimidazole (*IAZA), and radiofluorinated 1-#-D-(5-deoxy-5-[18F]-iodoarabinofuranosyl)-2-nitroimidazole (18FAZA). Such compounds are useful in imaging, therapy, or radiotherapy. Further, various syntheses of said precursors/synthons and the incorporation of said precursors/synthons into kits is provided. The precursors/synthons provided herein allow for an improved and facile manufacturing process for nitroimidazole-containing azomycin arabinosides.
• US8969546B2
  申请人：——

  公开号：US8969546B2

  公开（公告）日：2015-03-03
• [EN] COMPOUNDS USEFUL IN IMAGING AND THERAPY<br/>[FR] COMPOSÉS UTILES EN IMAGERIE ET EN THÉRAPIE
  申请人：UNIV ALBERTA

  公开号：WO2011160216A2

  公开（公告）日：2011-12-29

  As described herein there is provided novel precursors/synthons, and their chemical and radiochemical derivatives and methods of use thereof.