Preparation of 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) in ionic liquid, [bmim][OTf]

✍ Scribed by Byung Seok Moon; Kyo Chul Lee; Gwang Il An; Dae Yoon Chi; Seung Dae Yang; Chang Woon Choi; Sang Moo Lim; Kwon Soo Chun

• Publisher: John Wiley and Sons
• Year: 2006
• Tongue: French
• Weight: 128 KB
• Volume: 49
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1046

✦ Synopsis

Abstract

Although 3′‐deoxy‐3′‐[^18^F]fluorothymidine ([^18^F]FLT) is a prospective radiopharmaceutical for the imaging of proliferating tumor cell, it is difficult to prepare large amount of [^18^F]FLT. We herein describe the preparation of [^18^F]FLT in an ionic liquid, [bmim][OTf] (1‐butyl‐3‐methyl‐imidazolium trifluoromethanesulfonate). At optimized condition, [^18^F]fluorinationin ionic liquid with 5 µl of 1 M KHCO~3~ and 5 mg of the precursor yielded 61.5 ± 4.3% (n=10). Total elapsed time was about 70 min including HPLC purification. The rapid synthesis of [^18^F]FLT can be achieved by removing all evaporation steps. Overall radiochemical yield and radiochemical purity were 30 ± 5% and >95%, respectively. This method can use a small amount of a nitrobenzenesulfonate precursor and can be adapted for automated production. Copyright © 2006 John Wiley & Sons, Ltd.