(R,S)-anti-1-Amino-2-[18F]Fluorocyclopentyl-1-carboxylic Acid: Synthesis from Racemic 2-Benzyloxycyclopentanone and Biological Evaluation for Brain Tumor Imaging with P

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• 作者：Nachwa Jarkas ; Ronald J. Voll ; Larry Williams ; Vernon M. Camp ; Mark M. Goodman
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：September 23, 2010
• 年：2010
• 卷：53
• 期：18
• 页码：6603-6607
• 全文大小：735K
• 年卷期：v.53,no.18(September 23, 2010)
• ISSN：1520-4804

文摘

(R,S)-anti-1-Amino-2-fluorocyclopentyl-1-carboxylic acid (2-FACPC, 4b) was radiolabeled in 39% yield starting from cyclic sulfamidate 12. The 9L gliosarcoma cells assays showed that 4b is mainly a substrate for the L-type amino acid transport with some affinity to the A-type. In rats bearing 9L gliosarcoma tumors, 4b displayed high tumor to brain ratio (10:1) at 120 min after injection. FACPC is an attractive candidate for imaging brain tumors with PET, and its isolated enantiomers are under investigation.