Synthesis of tritium labelled CHS 828 and its prodrug EB 1627

被引：3

作者：

Schou, Søren Christian ^{[1
]}

Hunneche, Charlotte Schou ^{[1
]}

Binderup, Ernst ^{[1
]}

Grue-Sørensen, Gunnar ^{[1
]}

机构：

[1] Medicinal Chemistry Research, LEO Pharma, DK-2750 Ballerup

来源：

Journal of Labelled Compounds and Radiopharmaceuticals | 2005年 / 48卷 / 11期

关键词：

CHS; 828; EB; 1627; Pd/C catalysed tritiation; Prodrug; Tritio-debromination; Tritium;

D O I：

10.1002/jlcr.997

中图分类号：

TL [原子能技术];

学科分类号：

0827 ;

摘要：

The potent antitumoral cyanoguanidine CHS 828 and its prodrug EB 1627 have successfully been labelled with tritium. The pyridyl-3,5-dibromo derivative of CHS 828 was debrominated with tritium-gas using Pd/C catalyst to give [pyridyl-3,5-3H2]-CHS 828 with a radiochemical purity of 99.3% and a specific activity of 1960 GBq/ mmol. Similarly, the pyridyl-3-bromo derivative of the prodrug EB 1627 was debrominated with tritium-gas to give [pyridyl-3-3H]-EB 1627 with a radiochemical purity of 98.1% and a specific activity of 894 GBq/mmol. Copyright © 2005 John Wiley & Sons, Ltd.

引用

页码：789 / 795

页数：6

共 8 条

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