Synthesis of 3-Trimethylsilylbenzylguanidine as Precursor for <sup>125</sup>I Labeling

ZAN Liang-biao; YANG Yuan-you; LIU Ning; JIN Jian-nan; OU Xiao-hong

doi:10.7538/yzk.2007.41.06.0689

Atomic Energy Science and Technology > 2007 > 41(6): 689-693. > DOI: 10.7538/yzk.2007.41.06.0689

ZAN Liang-biao, YANG Yuan-you, LIU Ning, JIN Jian-nan, OU Xiao-hong. Synthesis of 3-Trimethylsilylbenzylguanidine as Precursor for ¹²⁵I Labeling[J]. Atomic Energy Science and Technology, 2007, 41(6): 689-693. DOI: 10.7538/yzk.2007.41.06.0689

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Synthesis of 3-Trimethylsilylbenzylguanidine as Precursor for ¹²⁵I Labeling

1.
Key Laboratory of Radiation Physics and Technology, Ministry of Education, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064, China
2.
Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu 610041, China

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Received Date: July 10, 2006
Revised Date: November 30, 2006

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Abstract

3-trimethylsilylbenzylguanidine, a precursor for ^125,131IMIBG or ²¹¹At MABG was synthesized in five steps using 3-bromotoluene as starting materials, and was characterized by NMR, MS and HPLC. With this precursor, free-carrier 125IMIBG was obtained with a labeling yield of 66.7% and radiochemical purity of more than 98% after purified using HPLC. Even stayed for 3 d at room temperature, the ¹²⁵I-MIBG maintains constantly stable in vitro, with radiochemical purity of more than 95%.
- 3-trimethylsilylbenzylguanidine,
- synthesis,
- ^125,131I,
- labeling

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[1]	WIELAND D M, BROWN L E, TOBES M C. Imaging the primate adrenal medulla with ¹²³I and ¹³¹I meta iodobenzylguanidine, concise communication[J]. J Nucl Med, 1981, 22: 358-364.
[2]	WIELAND D M, WU J L, BROWN L E, et al. Radiolabeled adrenergic neuronblocking agents：Adrenomedullary imaging with ¹³¹I iodibenzylguanidine[J]. J Nucl Med, 1980, 21: 349-353.
[3]	SHINODA M, SUZUKI Y, OI S, TSUGANE R, et al. Detection of norepinephrine distribution in rats with adrenal medulla autotransplants using¹²⁵I metaiodobenzyl guanidine[J]. Nucl Med Commun, 1994, 15: 752-757.
[4]	HOEFNAGEL C A, KRAKER J D, VALDES OLMOS R A, et al. ¹³¹IMIBFG as a firstline treatment in high risk neuroblastoma patients[J]. Nucl Med Commun, 1994, 15: 712-717.
[5]	BEIERWALTES W H. Applictions of ¹³¹Imiodobenzylguanidine ¹³¹I MIBG [J]. Nucl Med Biol, 1987, 14(3): 183-189.
[6]	CLARK H A, GORDON A F, YOUNG C W, et al. Position isomers of substituted aryl trimethyl silanes[J]. J Am Chem Soc, 1951, 73: 3 798-3 803.
[7]	SEVERSON R G, ROSSCUP R J, LINDBERG D R, et al. Substituted phenylsilanes：Ⅱ the bromination of the tolyltrimethylsilanes[J]. J Am Chem Soc, 1957, 79: 6 540-6 542.
[8]	GERTNER D, BOSEN H, ZILKHA A. Syntheses of some siliconcontaining βanimo acids[J]. Israel Journal of Chemistry, 1965/66, 3: 235-238.
[9]	VAIDYANATHAN G, ZALUTSKY M R. Nocarrieradded synthesis of meta[¹³¹I] iodobenzylguanidine[J]. Appl Radiat Isot, 1993, 44(3): 621-628.

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Synthesis of 3-Trimethylsilylbenzylguanidine as Precursor for 125I Labeling

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Synthesis of 3-Trimethylsilylbenzylguanidine as Precursor for ¹²⁵I Labeling