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

• DOI: 10.1021/acs.orglett.6b03730
• Publication Date: 2017-01-13T18:57:21Z
• Authors: Tanatorn Khotaviv...; Samuel Calderwood; Stefan Verhoog; Lukas Pfeifer; Sean Preshlock; Neil Vasdev; Thomas L. Collier; Véronique Gouverneur
• Keywords: Reactivity; Surface Modification

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 18F-difluoromethoxyarene, value approach is further demonstrated with coupling processes leading representative 18F-labeled TRPV1 inhibitors antagonists.