10.1002/jlcr.1502
The research aims to develop 18F-labeled vorozole analogues as PET tracers for detecting the enzyme aromatase, which converts androgens to estrogens and may influence mood and mental status. The study involves one- and two-step syntheses of two 18F-labeled vorozole analogues, [18F]FVOZ and [18F]FVOO, using key chemicals such as ethane-1,2-diyl bis(4-methylbenzenesulfonate), oxydiethane-2,1-diyl bis(4-methylbenzenesulfonate), and 1-bromo-2-fluoroethane. The one-step synthesis achieved higher radiochemical yields (36–99%) and specific radioactivities (100 GBq/mmol for [18F]FVOZ and 80 GBq/mmol for [18F]FVOO) compared to the two-step synthesis. In vitro autoradiography using frozen rat brains showed specific binding in regions corresponding to previous [11C]VOZ studies. Metabolite studies revealed that [18F]FVOZ was more stable in plasma than [18F]FVOO. The one-step synthesis method is highlighted as a more reproducible and potentially automatable approach for future tracer development.