The synthesis of radioiodinated 1-carboxamidino-4-phenylpiperazine

Zhentang Zhou; Yifang Ye; Yun Wang; Dequn Shen; Fasheng Fan; Yongchuan Wang; Qianmei Ji

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The synthesis of radioiodinated 1-carboxamidino-4-phenylpiperazine

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- The synthesis of radioiodinated 1-carboxamidino-4-phenylpiperazine
- Nuclear Techniques Vol. 08, Issue 9, (1985)
- 作者机构：
  
  中国科学院上海原子核研究所
- 作者简介：
- 基金信息：
- DOI：
  CLC：
- Received：24 April 1984，
  
  Published：1985-12
- 稿件说明：
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Zhentang Zhou, Yifang Ye, Yun Wang, et al. The synthesis of radioiodinated 1-carboxamidino-4-phenylpiperazine[J]. Nuclear techniques, 1985, 08(9): 31-32,54.
DOI：

Zhentang Zhou, Yifang Ye, Yun Wang, et al. The synthesis of radioiodinated 1-carboxamidino-4-phenylpiperazine[J]. Nuclear techniques, 1985, 08(9): 31-32,54. DOI：

摘要

肾上腺髓质和心肌显像的放射性药物研究颇受人们注视。1980年Wieland等

[1]

制备了放射性碘标记间碘苄胍（简称MIBG），在肾上腺显像方面取得较为满意的结果。1982年Hanson

[2]

报道了一个新的芳烷基胍的化合物——碘标记1－羧脒基－4－苯基哌嗪（简称

I-CPP），它对肾上腺亦有良好的选择性，且能快速标记和易于纯化。鉴于I-CPP有可能成为肾上腺髓质显像剂，故我们合成了重要中间体4－苯基哌嗪和研制了

131

I-CPP，以供药理和临床研究用。

Abstract

This report describes the synthesis of radioiodinated 1-carboxamidino-4-phenylpipera-zine——a new adrenomedullary imaging radiopharmaceutical.

To 4-phenylpiperazine in water a slight excess of s-methyl-thiouronium sulfide

was

added. The solution was heated at reflux for 6h and then cooled to room temperature

The precipitate formed was collected and recrystallized from hot water. This compound was radioiodinated by the chloramine-T method. The iodinated tracer was purified by paper chromatography. The yield was about 86% (from 83% to 89%). The radiochemical purity was over 98%.

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Keywords

references

D. M. Wieland et al ., J. Nucl. Med ., 21 , 349 （ 1980 ）.

R. N. Hanson , Int. J. Appl. Radiat. Isotopes , 33 , 629 （ 1982 ）.

U. S. A. patent Specification , 925, 218 （ 1960 ）.

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