Synthesis of 3H and 14C labeled (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indol-2-one, MaxiPoSt™.: An agent for post-stroke neuroprotection

被引：11

作者：

Dischino, DD

Gribkoff, VK

Hewawasam, P

Luke, GM

Rinehart, JK

Spears, TL

Starrett, JE

机构：

[1] Bristol Myers Squibb Co, Dept Chem Synth, Wallingford, CT 06492 USA

[2] Bristol Myers Squibb Co, Neurosci Drug Discovery, Wallingford, CT 06492 USA

[3] Bristol Myers Squibb Co, Neurosci Chem, Wallingford, CT 06492 USA

[4] Bristol Myers Squibb Co, Dept Chem Synth, Princeton, NJ 08540 USA

[5] Bristol Myers Squibb Co, Analyt Res & Dev, Wallingford, CT 06492 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2003年 / 46卷 / 02期

关键词：

neuroprotection; stroke; maxipost (TM); tritium; carbon-14;

D O I：

10.1002/jlcr.652

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The syntheses of tritium labeled (S)-3-(5-chloro-2-[(OCH3)-H-3]methoxyphenyl-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one, and carbon-14 (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-[2,3-C-14(2)] indol-2-one are reported. The H-3-labeled compound was prepared in a two-step synthesis from (CH3I)-H-3. The final product was purified via chiral HPLC to yield the desired enantiomer in a 4% radiochemical yield and a specific activity of 60 Ci/mmol. The C-14-labeled compound was prepared in a four-step synthesis from diethyl [carboxylate-C-14(1,2)] oxalate. The final product was purified via chiral HPLC to yield the desired enantiomer in a 20% radiochemical yield and a specific activity of 28.4 muCi/mg. Copyright (C) 2002 John Wiley Sons, Ltd.

引用

页码：139 / 149

页数：11

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