2-(4'-hydroxyphenyl)-6-hydroxyimidazo[1,2-a]pyridine | 956500-15-5

• 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-(4'-hydroxyphenyl)-6-hydroxyimidazo[1,2-a]pyridine
• 英文别名: 2-(4-hydroxyphenyl)imidazo[1,2-a]pyridin-6-ol
• CAS: 956500-15-5
• 化学式: C₁₃H₁₀N₂O₂
• 分子量: 226.235
• InChiKey: LLEVBSPEOUODSV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  57.8
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-溴-3-氟丙烷 、 2-(4'-hydroxyphenyl)-6-hydroxyimidazo[1,2-a]pyridine 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 24.0h， 生成 6-(3'-fluoropropoxy)-2-(4'-hydroxyphenyl)imidazo[1,2-a]pyridine
  参考文献：
  名称：

  NOVEL COMPOUND HAVING AFFINITY TO AMYLOID

  摘要：

  公开号：

  EP2022792B1
• 作为产物：
  描述：

  2-(4'-benzoyloxyphenyl)-6-methoxyimidazo[1,2-a]pyridine 在 三溴化硼 、 甲醇 作用下， 以 二氯甲烷 、 氯仿 为溶剂， 反应 20.0h， 生成 2-(4'-hydroxyphenyl)-6-hydroxyimidazo[1,2-a]pyridine
  参考文献：
  名称：

  NOVEL COMPOUND HAVING AFFINITY TO AMYLOID

  摘要：

  公开号：

  EP2022792B1

文献信息

• USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME
  申请人：Nihon Medi-Physics Co., Ltd.

  公开号：EP2216051A1

  公开（公告）日：2010-08-11

  The invention provides a reagent for detecting amyloid in a biological tissue which can detect amyloid in vitro and in vivo with high sensitivity using a compound which has affinity with amyloid and is suppressed in toxicity such as mutagenicity. The reagent for detecting amyloid deposited in a biological tissue comprises the compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, and R3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A3, A3 and A4 represents a carbon, and R5 binds to a carbon represented by A1, A2, A3 or A4.

  该发明提供了一种用于检测生物组织中淀粉样物质的试剂，该试剂可以使用一种具有与淀粉样物质亲和力且毒性抑制的化合物在体内和体外高灵敏度地检测淀粉样物质。用于检测生物组织中沉积淀粉样物质的试剂包括以下式（1）所表示的化合物或其盐：其中A1、A2、A3和A4独立地表示碳或氮，R3是由以下式表示的基团：其中R1是放射性卤素取代基；m是0至4的整数；n是0或1的整数，但至少有一个A1、A2、A3和A4表示碳，且R5与A1、A2、A3或A4表示的碳结合。
• Novel Compound Having Affinity For Amyloid
  申请人：Tanifuji Shigeyuki

  公开号：US20100092387A1

  公开（公告）日：2010-04-15

  A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R 1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R 2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.

  提供了一种与淀粉样物质具有亲和力、从正常组织中清除速度足够快且毒性被抑制（例如突变毒性）的化合物，该化合物由以下式子（1）表示：或其盐，其中R1是从氢、羟基、羧基、硫酸基、氨基、硝基、氰基、具有一到四个碳原子的烷基取代基或具有一到四个碳原子的烷氧基取代基中选择的基团；R2是放射性卤素取代基；m是0到2的整数。还提供了一种低毒性的阿尔茨海默病诊断剂，其包括上述式子或其盐所表示的化合物。
• Compound having affinity for amyloid
  申请人：Nihon Medi-Physics Co., Ltd.

  公开号：US08277777B2

  公开（公告）日：2012-10-02

  A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.

  提供了一种与淀粉样物质具有亲和力、从正常组织中清除速度足够快且毒性被抑制，其由以下式子（1）表示：或其盐，其中R1是从氢、羟基、羧基、硫酸基、氨基、硝基、氰基、1至4个碳原子的烷基取代基或1至4个碳原子的烷氧基取代基中选择的基团；R2是放射性卤素取代基；m是0至2的整数，还提供了一种低毒性的阿尔茨海默病诊断剂，其包括上述式子或其盐所表示的化合物。
• Novel Compound Having Affinity to Amyloid
  申请人：Tanifuji Shigeyuki

  公开号：US20100249407A1

  公开（公告）日：2010-09-30

  The invention relates to a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagenicity, and also relates to a low-toxic diagnostic agent for Alzheimer's disease containing the compound. The compound is represented by the following formula (1) or a salt thereof: wherein A 1 , A 2 , A 3 and A 4 independently represent a carbon or a nitrogen, and R 3 is a group represented by the following formula: wherein R 1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A 1 , A 2 , A 3 and A 4 represents a carbon, and R 3 binds to a carbon represented by A 1 , A 2 , A 3 or A 4 .

  本发明涉及一种与淀粉样物质亲和力强、从正常组织中清除速度足够快且毒性被抑制（例如突变原性），以及一种含有该化合物的低毒性诊断剂，用于阿尔茨海默病。该化合物由以下式（1）或其盐表示：其中，A1、A2、A3和A4独立地表示碳或氮，R3是由以下式表示的基团：其中，R1是放射性卤素取代基；m是0至4的整数；n是0或1的整数，但至少有一个A1、A2、A3和A4表示碳，且R3与A1、A2、A3或A4表示的碳结合。
• Compound having affinity to amyloid
  申请人：Nihon Medi-Physics Co., Ltd.

  公开号：US08022207B2

  公开（公告）日：2011-09-20

  The invention relates to a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagenicity, and also relates to a low-toxic diagnostic agent for Alzheimer's disease containing the compound. The compound is represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represent a carbon or a nitrogen, and R3 is a group represented by the following formula: wherein R1 is a radioactive halogen substituent; m is an integer of 0 to 4; and n is an integer of 0 or 1, provided that at least one of A1, A2, A3 and A4 represents a carbon, and R3 binds to a carbon represented by A1, A2, A3 or A4.

  本发明涉及一种具有与淀粉样物质亲和力、从正常组织中快速清除并且毒性被抑制，如致突变性的化合物，以及一种含有该化合物的低毒性阿尔茨海默病诊断剂。该化合物由以下式（1）或其盐表示：其中A1、A2、A3和A4独立地代表碳或氮，R3是由以下式表示的基团：其中R1是放射性卤素取代基；m为0到4的整数；n为0或1的整数，但至少有一个A1、A2、A3和A4代表碳，并且R3结合到由A1、A2、A3或A4表示的碳上。