Automated synthesis of 4-[F-18]fluoroanisole, [F-18]DAA1106 and 4-[F-18]FPhe using Cu-mediated radiofluorination under minimalist conditions

The application of the minimalist approach to Cu-mediated radiofluorination allows the efficient preparation of F-18-labeled arenes regardless of their electronic properties. The implementation of this methodology on a commercially available synthesis module (hotboxthree, Scintomics, Germany) enabled the automated production of 4-[F-18]fluoroanisole as well as the clinically relevant PET-tracers, 4-[F-18]FPhe and [F-18]DAA1106, in radiochemical yields of 41-61% and radiochemical purities of > 95% within 30-60 min. These results demonstrated the high efficacy and versatility of the developed method that will open up opportunities for a broad application of Cu-mediated radiofluorination in PET-chemistry. (C) 2016 Elsevier Ltd. All rights reserved