Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer <sup>131</sup>I-CLINDE

LI Bin1 LI Jianfeng2 WANG Xuebin3 HUANG Gang1; 4 1

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Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer ¹³¹I-CLINDE

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- Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer ¹³¹I-CLINDE
- NUCLEAR TECHNIQUES Issue 10, (2006)
- 作者机构：
  
  1. 上海交通大学医学院仁济医院核医学科
  2. 中国科学院上海生命科学院上海药物研究所
  3. 北京师范大学化学系
- 作者简介：
- 基金信息：
  
  上海市卫生局百人计划项目(97BR012);上海市教委重点发展基金(04BA03)资助
- DOI：
  CLC： R817
- Published：01 October 2006
- 稿件说明：
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[1]李斌,李剑峰,王学斌,黄钢.外周苯二氮卓受体示踪剂~(131)I-CLINDE的合成和标记[J].核技术,2006(10):777-781.

LI Bin1 LI Jianfeng2 WANG Xuebin3 HUANG Gang1, 4 1. Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer ¹³¹I-CLINDE[J]. Nuclear techniques, 2006, (10): 777-781.
[1]李斌,李剑峰,王学斌,黄钢.外周苯二氮卓受体示踪剂~(131)I-CLINDE的合成和标记[J].核技术,2006(10):777-781. DOI：

LI Bin1 LI Jianfeng2 WANG Xuebin3 HUANG Gang1, 4 1. Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer ¹³¹I-CLINDE[J]. Nuclear techniques, 2006, (10): 777-781. DOI：

摘要

本文报道CLINDE改进的合成方法及其同位素131I-标记。标记前体由5-氯-2-氨基吡啶与溴代酮酰胺缩合制得。标记产物经三烷基锡化、过氧化氢-碘脱锡化而得。产物经反向HPLC分离纯化。结果显示

标记前体总收率30.8%

标记物放化得率80%

TLC和HPLC检测放化纯度大于98%。表明该法简便易行

放化得率好

产物纯度（包括放射化学纯度）高。

Abstract

This paper describes the preparation of N

N’-diethyl-6-chloro-(4’-iodophenyl)-imidazo-[1

2-a] pyridine-3-acetamide (CLINDE) and [131I]- labelled ([131I]- CLINDE). Non-radioactive imidazo[1

2-a]pyridine was synthesized by condensation of 5-chloro-2-aminopyridines with the bromo keto amides. Radiolabelling [131I]- imidazo [1

2-a]pyridines was prepared by iododestannylation with Na[131I] in the presence of peroxide of hydrogen and purified by C18 reverse phase HPLC. Non-radioactive imidazo-[1

2-a] pyridine was synthesized at a total yield of 30.8%. Radiolabelling [131I]-imidazo [1

2-a]pyridines was prepared with a radiochemical yield of 80% and a radiochemical purity of greater than 98%. An improved

economical process is suited for preparing N

N’-diethyl-6-chloro-(4’-iodo-phenyl)-imidazo-[1

2-a]pyridine-3-acetamide and its radiosynthesis.

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Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer 131I-CLINDE

DOI：

摘要

Abstract

关键词

Keywords

references

Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer ¹³¹I-CLINDE