2-[4'-(3''-t-butyldimethylsiloxypropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine | 958641-90-2

• 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'-(3''-t-butyldimethylsiloxypropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine
• 英文别名: tert-butyl-[3-[4-(6-iodoimidazo[1,2-a]pyridin-2-yl)phenoxy]propoxy]-dimethylsilane
• CAS: 958641-90-2
• 化学式: C₂₂H₂₉IN₂O₂Si
• 分子量: 508.474
• InChiKey: KSDVKWDDTYEACX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.4
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  35.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-[4'-(3''-t-butyldimethylsiloxypropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine 在 四丁基氟化铵 、 水 、 氯化铵 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 0.5h， 生成 2-[4-(3-hydroxypropoxy)phenyl]-6-iodoimidazo[1,2-a]pyridine
  参考文献：
  名称：

  COMPOUND HAVING AFFINITY FOR AMYLOID

  摘要：

  公开号：

  EP2019103B1
• 作为产物：
  描述：

  2-(4-hydroxyphenyl)-6-iodoimidazo[1,2-a]pyridine 、 (3-溴丙氧基)叔丁基二甲基硅烷 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 192.0h， 生成 2-[4'-(3''-t-butyldimethylsiloxypropoxy)phenyl]-6-iodoimidazo[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：US20100069640A1

  公开（公告）日：2010-03-18

  A compound represented by the following formula or a salt thereof: wherein each of A 1 , A 2 , A 3 and A 4 independently represents a carbon or nitrogen, R 1 is a radioactive halogen substituent, R 2 is a group selected from the group consisting of hydrogen, a hydroxyl group, a methoxy group, a carboxyl group, an amino group, an N-methylamino group, an N,N-dimethylamino group and a cyano group, and p is an integer of 0 to 2, provided 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 , is effective as an image diagnosis probe targeting amyloid and a diagnostic agent for Alzheimer's disease.

  以下化合物或其盐，其化学式如下： 其中，每个A1、A2、A3和A4独立地代表碳或氮，R1是一个放射性卤素取代基，R2是从氢、羟基、甲氧基、羧基、氨基、N-甲基氨基、N,N-二甲基氨基和氰基组成的一组基团，p是0到2的整数，至少有一个A1、A2、A3和A4代表碳，且R1结合到由A1、A2、A3或A4代表的碳上，其作为靶向淀粉样蛋白的影像诊断探针和阿尔茨海默病诊断剂具有有效性。
• 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。
• UTILIZATION OF NOVEL COMPOUNDS WITH AMYLOID AFFINITY AND METHOD OF PRODUCING THE SAME
  申请人：Tanifuji Shigeyuki

  公开号：US20100249419A1

  公开（公告）日：2010-09-30

  The invention provides a reagent for detecting amyloid deposited 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 mutagencity. The reagent for detecting amyloid deposited in a biological tissue comprises a compound 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 nitrogen; R 1 is a radioactive halogen substituent; R 2 is a group selected from the group consisting of hydrogen, hydroxyl group, methoxy group, carboxyl group, amino group, N-methylamino group, N,N-dimethylamino group and cyano group; and m is an integer of 0 to 2, provided that 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 and A 4 .

  本发明提供了一种用于检测生物组织中沉积的淀粉样蛋白的试剂，该试剂使用与淀粉样蛋白具有亲和力且抑制毒性（如突变原性）的化合物，在体外和体内具有高灵敏度检测淀粉样蛋白。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独立地表示碳或氮；R1是放射性卤素取代基；R2是从氢、羟基、甲氧基、羧基、氨基、N-甲基氨基、N,N-二甲基氨基和氰基组成的群体中选择的一组基团；m是0到2的整数，前提是A1、A2、A3和A4中至少有一个表示碳，并且R1结合到由A1、A2、A3和A4表示的碳。
• Compound having affinity for amyloid
  申请人：Nihon Medi-Physics Co., Ltd.

  公开号：US08207189B2

  公开（公告）日：2012-06-26

  A compound represented by the following formula or a salt thereof: wherein each of A1, A2, A3 and A4 independently represents a carbon or nitrogen, R1 is a radioactive halogen substituent, R2 is a group selected from the group consisting of hydrogen, a hydroxyl group, a methoxy group, a carboxyl group, an amino group, an N-methylamino group, an N,N-dimethylamino group and a cyano group, and p is an integer of 0 to 2, provided 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, is effective as an image diagnosis probe targeting amyloid. A diagnostic agent for Alzheimer's disease contains the compound.

  以下化合物公式或其盐：其中，A1、A2、A3和A4中的每一个独立地表示碳或氮，R1是放射性卤素取代基，R2是从氢、羟基、甲氧基、羧基、氨基、N-甲基氨基、N,N-二甲基氨基和氰基组成的群体中选择的一种，p是0到2的整数，至少A1、A2、A3和A4中的一个表示碳，且R1与A1、A2、A3或A4表示的碳结合，可作为靶向淀粉样蛋白的影像诊断探针。一种阿尔茨海默病诊断剂含有该化合物。