Precursor synthesis of molecular probe of estrogen receptor β and the <sup>99m</sup>Tc radiolabeling

ZHANG Chunchun1; 2 HUANG Liliang1; 2 ZHU Hua1; 2 SUN Yanhong1 ZHANG Yuanqing1; 2 XU Jia1 SHEN Yumei1 1

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Precursor synthesis of molecular probe of estrogen receptor β and the ^99mTc radiolabeling

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- Precursor synthesis of molecular probe of estrogen receptor β and the ^99mTc radiolabeling
- NUCLEAR TECHNIQUES Vol. 32, Issue 4, (2009)
- 作者机构：
  
  1. 中国科学院上海应用物理研究所,放射性药物研究中心
  2. 中国科学院研究生院
- 作者简介：
- 基金信息：
  
  中国科学院“百人计划”(26200601);中国科学院前沿领域项目(55200701)资助
- DOI：
  CLC： TQ467
- Published：01 April 2009
- 稿件说明：
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[1]张春春,黄立梁,朱华,孙艳红,张元庆,许嘉,沈玉梅.雌激素受体β分子探针前体的合成及~(99m)Tc标记[J].核技术,2009,32(04):303-308.

ZHANG Chunchun1, 2 HUANG Liliang1, 2 ZHU Hua1, et al. Precursor synthesis of molecular probe of estrogen receptor β and the ^99mTc radiolabeling[J]. Nuclear techniques, 2009, 32(4): 303-308.
[1]张春春,黄立梁,朱华,孙艳红,张元庆,许嘉,沈玉梅.雌激素受体β分子探针前体的合成及~(99m)Tc标记[J].核技术,2009,32(04):303-308. DOI：

ZHANG Chunchun1, 2 HUANG Liliang1, 2 ZHU Hua1, et al. Precursor synthesis of molecular probe of estrogen receptor β and the ^99mTc radiolabeling[J]. Nuclear techniques, 2009, 32(4): 303-308. DOI：

摘要

以对甲氧基苯甲醛和对甲氧基苯乙腈为起始原料

经羟醛缩合、乙烯基化、脱甲基化、甲氧甲基化、硼氢化-氧化、甲磺酰化、碘代、仲胺亲核取代、脱甲氧甲基化等步骤完成了一种用于显像雌激素受体β分子探针前体:（2R*

3S*）-5-[二（2-吡啶甲基）-胺基]-2

3-二（4-羟苯基）戊腈（9）的合成

总产率为8.2%。用[Et4N]2[Re（CO）3Br3]与之配位合成其冷标记铼配合物

并用99mTc对该前体进行放射化学标记

为其在乳腺癌肿瘤中ERβ的SPECT成像评估乳腺癌的恶化程度奠定了基础。产物通过1HNMR、IR、MS或元素分析进行了结构确证。

Abstract

(2R*

3S*)-5-[bis(2-pyridyl-methyl)-amino]-2

3-bis(4-hydroxyphenyl) pentanenitrile

a novel molecular probe precursor for imaging estrogen receptor β

was synthesized by the following procedures:condensation

vinylation

demethylation

methoxymethyl protection

hydroboration-oxidation

methane sulfonylation

iodination

substitution by secondary amine

deprotection starting from 4-methoybenzaldehyde and 4-methoxybenzyl cyanide.Its Re-tricarbonyl complex was synthesized with cold labeling.The precursor was radiolabeled with 99mTc successfully.The structures have been confirmed by 1H NMR

FTIR and MS characterization or elemental analysis.The study of help in the assessment of breast cancer stages by imaging ERβ with SPECT.

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Precursor synthesis of molecular probe of estrogen receptor β and the 99mTc radiolabeling

DOI：

摘要

Abstract

关键词

Keywords

references

Precursor synthesis of molecular probe of estrogen receptor β and the ^99mTc radiolabeling