Ring opening of epoxides with [¹⁸F]FeF species to produce [¹⁸F]fluorohydrin PET imaging agents

A simple technique for the preparation of [¹⁸F]HF has been developed and applied to the generation of an [¹⁸F]FeF species for opening sterically hindered epoxides. This method has been successfully employed to prepare four drug-like molecules, including 5-[¹⁸F]fluoro-6-hydroxy-cholesterol, a potential adrenal/endocrine PET imaging agent. This easily automated one-pot procedure produces sterically hindered fluorohydrin PET imaging agents in good yields and high molar activities.