...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Radiosynthesis of a carbon-11-labeled AMPAR allosteric modulator as a new PET radioligand candidate for imaging of Alzheimer's disease
【24h】

Radiosynthesis of a carbon-11-labeled AMPAR allosteric modulator as a new PET radioligand candidate for imaging of Alzheimer's disease

机译：碳-11标记的AMPAR颠振调制剂的可热覆盖合成作为阿尔茨海默病成像的新宠物放射性配体候选者

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

To develop PET tracers for imaging of Alzheimer's disease, a new carbon-11-labeled AMPAR allosteric modulator 4-cyclopropyl-7-(3-[C-11] methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4] thiadiazine 1,1-dioxide ([C-11] 8) has been synthesized. The reference standard 4-cyclopropyl-7-(3-methoxyphenoxy)-3,4-dihydro-2H-benzo[e][1,2,4] thiadiazine 1,1-dioxide (8) and its corresponding desmethylated precursor 4-cyclopropyl-7-(3-hydroxyphenoxy)3,4- dihydro-2H-benzo[e][1,2,4] thiadiazine 1,1-dioxide (9) were synthesized from 4-methoxyabiline and chlorosulfonyl isocyanate in eight and nine steps with 3% and 1% overall chemical yield, respectively. The target tracer [C-11] 8 was prepared from the precursor 9 with [C-11] CH3OTf through O-[C-11] methylation and isolated by HPLC combined with SPE in 10-15% radiochemical yield, based on [C-11] CO2 and decay corrected to end of bombardment (EOB). The radiochemical purity was> 99%, and the molar activity (AM) at EOB was 370-740 GBq/mu mol with a total synthesis time of 35-40-minutes from EOB.
机译：为了开发宠物跟踪器，用于成像阿尔茨海默病，一种新的碳-11标记的AMPAR颠振调制剂4-环丙基-7-（3- [C-11]甲氧基苯氧基）-3,4-二氢-2H-苯并[E] [ 1,2,4]噻二嗪1,1-二氧化物（[C-11] 8）已被合成。参考标准4-环丙基-7-（3-甲氧基苯氧基）-3,4-二氢-2H-苯并[e] [1,2,4]噻二嗪1,1-二氧化物（8）及其相应的去甲基化前体4-环丙基-7-（3-羟基苯氧基）3,4-二氢-2H-苯并[e] [1,2,4]噻二嗪1,1-二氧化噻吩（9）由4-甲氧基苯胺和氯磺酰基异氰酸酯合成八个和九个分别具有3％和1％的总体化学产率的步骤。通过通过[C-11] CH 3 O-[C-11]甲基化并通过HPLC与SPE分离的10-15％的放射化学产率分离，基于[C-11]，将靶示踪剂[C-11] 8用O-[C-11] CH 3 O-[C-11]甲基化制备。 -11] CO2和衰减纠正为轰炸（EOB）的结束。放射化学纯度> 99％，EOB的摩尔活性（AM）为370-740GBq / mumol，总合成时间为35-40分钟。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号