Rapid and reproducible radiosynthesis of [18F] FHBG.
9-(4-[18F] Fluoro-3-hydroxymethylbutyl) guanine ([18F] FHBG), an imaging agent for gene therapy using PET, was prepared in a one-pot, two-step synthesis. Microwave (MW) mediated nucleophilic fluorination of N2, monomethoxytrityl-9-[4-(tosyl)-3-monomethoxytrityl-methylbutyl] guanine using no-carrier-added [18F] fluoride, followed by deprotection with hydrochloric acid and HPLC purification, gave [18F] 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.
Ponde
Datta E
DE
Division of Radiological Sciences, Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 S. Kingshighway, MSt. Louis, MO 63110, USA.
Dence
Carmen S
CS
Schuster
Daniel P
DP
Welch
Michael J
MJ
D000818:Animals; D006147:Guanine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000493:pharmacokinetics*; D008168:Lung / Q000000981:diagnostic imaging* / Q000378:metabolism*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013937:Thymidine Kinase / Q000235:genetics / Q000378:metabolism*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed / Q000379:methods; D014764:Viral Proteins / Q000235:genetics / Q000378:metabolism*
C113308:9-(4-fluoro-3-hydroxymethylbutyl)guanine; D019275:Radiopharmaceuticals; D014764:Viral Proteins; D006147:Guanine; C099241:thymidine kinase, Canid herpesvirus 1; D013937:Thymidine Kinase