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9-(4-[F-18] Fluoro-3-hydroxymethylbutyl) guanine ([F-18] FHBG), an imaging agent for gene therapy using PET, was prepared in a one-pot, two-step synthesis. Microwave (MW) mediated nucleophilic fluorination of N-2, monomethoxytrityl-9-[4-(tosyl)-3-monomethoxytrityl-methylbutyl] guanine using no-carrier-added [F-18] fluoride, followed by deprotection with hydrochloric acid and HPLC purification, gave [F-18] FHBG. The radiochemical yield (decay corrected) was 12 +/- 5% (n = 35), the synthesis time was 55-60 min, and the radiochemical purity was >99%. The compound was used for lung imaging and was injected into Sprague-Dawley rats previously infected with the herpes simplex virus type 1 thymidine kinase (HSV1-tk) reporter gene. MicroPET imaging showed accumulation confined to the lungs. (C) 2004 Elsevier Inc. All rights reserved.