A new method for the preparation of 8-[18F]fluoroguanine derivatives based on a direct radiofluorination reaction has been developed. The radiofluorination of ganciclovir (1a) with [18F]F2 was carried out in absolute ethanol in the presence of tetraethylammonium hydroxide at room temperature to give 8-[18F]fluoroganciclovir (3a) in an approximately 1% radiochemical yield. Similarly, 8-[18F]fluoropenciclovir (3b), 8-[18F]fluoroacyclovir (3c), and 8-[18F]fluoroguanosine (3d) were synthesized from penciclovir (1b), acyclovir (1c), and guanosine (1d), respectively, using [18F]F2. The structural analyses of the final products (3a, 3b, 3c, and 3d) were carried out after 18F decay by 1H, 13C, and 19F nuclear magnetic resonance and high resolution mass spectroscopy. Copyright (C) 2000 Elsevier Science Inc.
- Gene expression
ASJC Scopus subject areas
- Cancer Research
- Molecular Medicine
- Radiology Nuclear Medicine and imaging