6-bromo-2-[4'-(3''-fluoropropoxy)phenyl]imidazo[1,2-a]pyridine | 958641-67-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 6-bromo-2-[4'-(3''-fluoropropoxy)phenyl]imidazo[1,2-a]pyridine
• 英文别名: 6-bromo-2-[4-(3-fluoropropoxy)phenyl]imidazo[1,2-a]pyridine
• CAS: 958641-67-3
• 化学式: C₁₆H₁₄BrFN₂O
• 分子量: 349.202
• InChiKey: YHHGLIPKAMQMBD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  21
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  26.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-bromo-2-[4'-(3''-fluoropropoxy)phenyl]imidazo[1,2-a]pyridine 、 六正丁基二锡 在 三苯基膦钯 三乙胺 作用下， 以 1,4-二氧六环 为溶剂， 生成 6-tributylstannyl-2-[4'-(3'-fluoropropoxy)phenyl]imidazo[1,2-a]pyridine
  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：

  1-溴-3-氟丙烷 、 6-bromo-2-(4 - hydroxyphenyl)imidazo[1,2-a]pyridine 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 20.5h， 生成 6-bromo-2-[4'-(3''-fluoropropoxy)phenyl]imidazo[1,2-a]pyridine
  参考文献：
  名称：

  COMPOUND HAVING AFFINITY FOR AMYLOID

  摘要：

  公开号：

  EP2019103B1

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：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 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。