[18F]Fluoropropylsulfonyl chloride: a new reagent for radiolabeling primary and secondary amines for PET imaging

✍ Scribed by Zheng Li; Lixin Lang; Ying Ma; Dale O. Kiesewetter

• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: French
• Weight: 167 KB
• Volume: 51
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1466

✦ Synopsis

Abstract

In vivo molecular imaging with positron emission tomography (PET) requires the preparation of an appropriate positron‐emitting radiotracer. New methods for the introduction of F‐18 into biologically interesting molecules could increase the availability of specific PET radiotracers and increase the application of PET to the study of human diseases. In this work, [^18^F]fluoropropylsulfonyl chloride was synthesized from 3‐toluenesulfonyloxypropyl thiocyanate in two steps and was successfully incorporated into molecules containing a reactive amino group. Both a primary amine, L‐phenylalanine ethyl ester hydrochloride, and a secondary amine, 1‐(2‐methoxyphenyl)‐piperazine, were successfully radiolabeled by this method. The entire radiochemical synthesis required 90 min. The products were obtained in 25.7±2.3% (n=3) and 22.8±9.1% (n=6) (EOB). This method provides a useful and easy way to make new F‐18 labeled radiopharmaceuticals for PET imaging. Copyright © 2008 John Wiley & Sons, Ltd.