Radiosyntheses of 3-{[4-(4-[<sup>18</sup>F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine

TIAN Haibin  YIN Duanzhi  ZHANG Lan  ZHANG Chunfu   LI Junling  ZHOU Wei  WANG Yongxian

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Radiosyntheses of 3-{[4-(4-[¹⁸F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine

更新时间：2021-03-12

- Radiosyntheses of 3-{[4-(4-[¹⁸F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine
- NUCLEAR TECHNIQUES Issue 8, (2003)
- 作者机构：
  
  1. 中国科学院上海原子核研究所
  2. 中国科学院上海原子核研究所,上海,201800
- 作者简介：
- 基金信息：
  
  中国科学院创新工程重大项目(KJCXI-SW-08)资助
- DOI：
  CLC： O615
- Published：01 August 2003
- 稿件说明：
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[1]田海滨,尹端沚,张岚,张春富,李俊玲,周伟,汪勇先.3-[4-(4-[~(18)F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶的放射化学合成[J].核技术,2003(08):628-632.

TIAN Haibin YIN Duanzhi ZHANG Lan ZHANG Chunfu LI Junling ZHOU Wei WANG Yongxian. Radiosyntheses of 3-{[4-(4-[¹⁸F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine[J]. Nuclear techniques, 2003, (8): 628-632.
[1]田海滨,尹端沚,张岚,张春富,李俊玲,周伟,汪勇先.3-[4-(4-[~(18)F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶的放射化学合成[J].核技术,2003(08):628-632. DOI：

TIAN Haibin YIN Duanzhi ZHANG Lan ZHANG Chunfu LI Junling ZHOU Wei WANG Yongxian. Radiosyntheses of 3-{[4-(4-[¹⁸F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine[J]. Nuclear techniques, 2003, (8): 628-632. DOI：

摘要

L-750

667是具有高亲和性（Ki= 0.51 nmol/L）的D4受体选择性配体

采用一锅法用氟[18F]化物放射化学合成了L-750

667的类似物:3-[4-（4-[18F]氟苯甲基）哌嗪-1-基]-甲基-1H-吡咯并[2

3-b]吡啶。4-氟[18F]苯甲醛是由无载体的 [18F]F-与标记前体4-三甲基铵苯甲醛-三氟甲基磺酸盐在DMSO中反应获得。在同一容器中

4-氟[18F]苯甲醛和3-（哌嗪-1-基）甲基-1H-吡咯并[2

3-b]吡啶完成胺烷基化反应得到产物。产物的纯化使用HPLC

产物保留时间tR=9.4min。在同一条件下

确定产物的放化纯度。放化产率为12.0%

放化纯度>98%

比活度高于37GBq/μmol

全部合成时间（包括高效液相分离）为73min。制备的产物可作为潜在的多巴胺D4受体正电子发射断层（PET）显像剂。

Abstract

L-750

667 is a novel

high-affinity (Ki = 0.51 nmol/L) and selective D4 receptor ligand. A L-750

667 analogue

3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl}methyl-1H-pyrrolo[2

3-b]pyridine

was prepared by reacting 3- (piperazin-1-yl)-methyl-1H-pyrrolo[2

3-b]pyridine with 4-[18F]fluorobenzaldehyde. The 4-[18F] fluorobenzaldehyde was prepared by nucleophilic substitution using no carrier added [18F]fluoride from trimethylammonium- benzaldehyde triflate in DMSO. The radiochemical yield of 3-{[4-(4-[18F]fluorobenzyl)] piperazin-1-yl}methyl-1H- pyrrolo[2

3-b]pyridine was 12.0% (decay –corrected) with a radiochemical purity better than 98% and a specific activity greater than 37GBq/mmol

and the synthesis time including HPLC purification was 73 min. This labeled compound may be a useful PET tracer for dopamine D4 receptors.

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Radiosyntheses of 3-{[4-(4-[18F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine

DOI：

摘要

Abstract

关键词

Keywords

references

Radiosyntheses of 3-{[4-(4-[¹⁸F]fluorobenzyl)]piperazin-1-yl} methyl-1H-pyrrolo[2,3-b]pyridine