Microwave-assisted synthesis and chiral HPLC separation of 18F-labeled MaxiPost™.: An agent for post-stroke neuroprotection

被引：5

作者：

Dischino, DD ^{[1
]}

Dulac, HA ^{[1
]}

Gillman, KW ^{[1
]}

Keller, LS ^{[1
]}

Kozlowski, ES ^{[1
]}

Marcin, LR ^{[1
]}

Mongillo, JJ ^{[1
]}

Starrett, JE ^{[1
]}

机构：

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

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2003年 / 46卷 / 12期

关键词：

neuroprotection; stroke; MaxiPost (TM); F-18; microwave;

D O I：

10.1002/jlcr.748

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

The syntheses of (S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-[F-18]-fluoro-6-(trifluoromethyl)-1H-indol-2-one was accomplished by the microwave assisted carrier-added 18F fluorination of (R, S)-3-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-chloro-6-(trifluoromethyl)-1H-indol-2-one, followed by chiral HPLC separation to afford the desired 18 F-labeled enantiomer in radiochemical yields of 5-15% (EOS) and synthesis and purification times of 60-67 min. Biodistribution studies in rodents were consistent with previously reported studies using racemic F-18-radiolabeled material. Copyright (C) 2003 John Wiley Sons, Ltd.

引用

页码：1161 / 1171

页数：11

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