Asymmetric (18)F-fluorination for applications in positron emission tomography

Positron emission tomography (PET) is becoming more frequently used by medicinal chemists to facilitate the selection of the most promising lead compounds for further evaluation. For PET, this entails the preparation of (11)C- or (18)F-labeled drugs or radioligands. With the importance of chirality and fluorine substitution in drug development, chemists can be faced with the challenge of preparing enantiopure molecules featuring the (18)F-tag on a stereogenic carbon. Asymmetric (18)F-fluorination is an emerging field of research that provides an alternative to resolution or conventional S(N)2-based radiochemistry. To date, both transition metal complexes and organomediators have been successfully employed for (18)F-incorporation at a stereogenic carbon.