Synthesis and Reactivity of 18F-Labeled α,α-Difluoro-α-(aryloxy)acetic Acids

Article abstract of DOI:10.1021/acs.orglett.6b03730

In this work, we describe the ¹⁸F-labeling of α,α-difluoro-α-(aryloxy)acetic acid derivatives and demonstrate that these building blocks are amenable to post-¹⁸F-fluorination functionalization. Protodecarboxylation offers a new entry to ¹⁸F-difluoromethoxyarene, and the value of this approach is further demonstrated with coupling processes leading to representative ¹⁸F-labeled TRPV1 inhibitors and TRPV1 antagonists.