A Cu(I)-mediated
fluoro-deamination method for nucleophilic radiofluorination
was devised. The method affords fluorinated aromatic products directly
from anilines under both no-carrier added and stoichiometric conditions.
Isolated radiochemical yields range from 11% to 81% with high radiochemical
purities and a molar activity of 58 MBq/nmol. The reaction conditions
were implemented successfully in an automated process for production
of (
S
)-4[
18
F]fluorogluthetimide on a radiosynthesis
module.
A tris(pentafluorophenyl)borane catalysed method for the synthesis of boronic acid esters from aromatic amines in yields of up to 93% was devised. Mild conditions, benign reagents, short reaction times, low temperatures and a wide substrate scope characterize the method. The reaction was found applicable to the synthesis of boronic acid ester derivatives of complex drug molecules in up to 86% isolated yield and high purity suitable for labelling. These boronates were subsequently labelled with [18F]fluoride ion in radiochemical yields of up to 55% with and even without isolation of the boronate-intermediate.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.