2-(4'-hydroxyphenyl)-6-iodoimidazo[1,2-a]pyrimidine | 956499-77-7

• 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-iodoimidazo[1,2-a]pyrimidine
• 英文别名: 4-(6-iodoimidazo[1,2-a]pyrimidin-2-yl)phenol
• CAS: 956499-77-7
• 化学式: C₁₂H₈IN₃O
• 分子量: 337.12
• InChiKey: GLKDFGAOWZETRP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 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：
  50.4
• 氢给体数：
  1
• 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-iodoimidazo[1,2-a]pyrimidine 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 2-[4'-(3'-fluoropropoxy)phenyl]-6-iodoimidazo[1,2-a]pyrimidine
  参考文献：
  名称：

  USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME

  摘要：

  该发明提供了一种用于检测生物组织中淀粉样蛋白的试剂，可以利用一种与淀粉样蛋白亲和力强且在毒性方面受到抑制（如致突变性）的化合物，在体外和体内高灵敏度地检测淀粉样蛋白。用于检测生物组织中沉积的淀粉样蛋白的试剂包括下式（1）所表示的化合物或其盐：其中A1、A2、A3和A4独立地代表碳或氮；R1是卤素取代基；R2是卤素取代基；m是整数或0到2，但至少R1和R2中的一个是放射性卤素取代基，A1、A2、A3和A4中至少一个代表碳，且R1与A1、A2、A3和A4所代表的碳结合。

  公开号：

  EP2218463A1
• 作为产物：
  描述：

  2-氨基-5-碘嘧啶, 、 2-溴-4'-羟基苯乙酮 在 乙腈 、 碳酸氢钠 、 水 作用下， 以 乙腈 为溶剂， 反应 8.05h， 以to obtain 737 mg (corresponding to 2.19 mmol) of 2-(4′-hydroxyphenyl)-6-iodoimidazo[1,2-a]pyrimidine (FIG. 1-8, Step 2)的产率得到2-(4'-hydroxyphenyl)-6-iodoimidazo[1,2-a]pyrimidine
  参考文献：
  名称：

  USE OF NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID, AND PROCESS FOR PRODUCTION OF THE SAME

  摘要：

  本发明提供了一种检测生物组织中淀粉样物质的试剂，该试剂使用与淀粉样物质亲和力强且毒性低（如突变原性）的化合物，可以高灵敏度地在体内外检测淀粉样物质。检测生物组织中沉积的淀粉样物质的试剂包括下式（1）所表示的化合物或其盐：其中，A1、A2、A3和A4独立表示碳或氮，R3是下式所表示的基团：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表示碳，并且R3与A1、A2、A3或A4表示的碳结合。

  公开号：

  US20100249408A1

文献信息

• Novel Compound Having Affinity for Amyloid
  申请人：Tanifuji Shigeyuki

  公开号：US20090252679A1

  公开（公告）日：2009-10-08

  The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A 1 , A 2 , A 3 and A 4 independently represents a carbon or nitrogen; R 1 is a halogen substituent; R 2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R 1 and R 2 is a radioactive halogen substituent, at least one of A 1 , A 2 , A 3 and A 4 represents a carbon, and R 1 binds to a carbon represented by A 1 , A 2 , A 3 or A 4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.

  本发明提供了一种与淀粉样蛋白亲和力强，从正常组织中清除速度足够快且毒性（如诱变性）被抑制的化合物。所提供的化合物由以下公式（1）或其盐所表示：其中，A1、A2、A3和A4独立地表示碳或氮；R1是卤素取代基；R2是卤素取代基；m是0到2的整数，但至少其中一个R1和R2是放射性卤素取代基，至少一个A1、A2、A3和A4表示碳，且R1与由A1、A2、A3或A4表示的碳结合，以及包含由上述公式或其盐所表示的低毒性诊断剂。
• NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID
  申请人：TANIFUJI Shigeyuki

  公开号：US20120271053A1

  公开（公告）日：2012-10-25

  The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A 1 , A 2 , A 3 and A 4 independently represents a carbon or nitrogen; R 1 is a halogen substituent; R 2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R 1 and R 2 is a radioactive halogen substituent, at least one of A 1 , A 2 , A 3 and A 4 represents a carbon, and R 1 binds to a carbon represented by A 1 , A 2 , A 3 or A 4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.

  本发明提供了一种与淀粉样物质亲和力较强、从正常组织中清除速度足够快且毒性如突变原性得到抑制的化合物。提供的化合物由以下公式（1）或其盐表示：其中，A1、A2、A3和A4独立地表示碳或氮；R1是卤素取代基；R2是卤素取代基；m是0到2的整数，但至少R1和R2中的一个是放射性卤素取代基，至少A1、A2、A3和A4中的一个表示碳，且R1结合到由A1、A2、A3或A4表示的碳，以及包含上述公式或其盐所表示的化合物的低毒性诊断剂。
• Alkoxy substituted imidazo[1,2-a]pyridines having affinity for amyloid
  申请人：Nihon Medi-Physics Co., Ltd.

  公开号：US08303935B2

  公开（公告）日：2012-11-06

  The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.

  本发明提供了一种与淀粉样蛋白亲和力强，从正常组织中清除速度足够快且毒性抑制，例如突变性的化合物。提供了一种由以下式(1)或其盐所表示的化合物：其中A1、A2、A3和A4独立地代表碳或氮；R1是卤素取代基；R2是卤素取代基；m是0到2的整数，前提是R1和R2中至少有一个是放射性卤素取代基，A1、A2、A3和A4中至少有一个代表碳，R1结合到由A1、A2、A3或A4所代表的碳，以及包含上述式或其盐所表示的低毒诊断剂的方法。
• 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。