Enzymatic radiofluorination: Fluorinase accepts methylaza-analog of SAM as substrate for FDA synthesis

•Novel substrate, methylaza-analog of SAM, was suggested for fluorinase-catalyzed radiofluorination.•Optimal reaction conditions are established.•MeAzaAdoMet was fluorinated with [18F]F− ions with 32% yield.

Methylaza-analog of S-adenosyl-l-methionine (MeAzaAdoMet) was found to be a substrate for fluorinase. This is the first discovery of a new substrate for fluorinase that can be accessed synthetically in high purity. The activity of fluorinase for the new MeAzaAdoMet and [18F]fluoride ion was 32% in 180 min.

Graphical abstractApplication of methylaza-analog of S-adenosyl-l-methionine (MeAzaAdoMet) as a substrate for fluorinase is described. Optimal radiofluorination conditions are established and the desired [18F]FDA is obtained with 32% yield in 180 min.Figure optionsDownload full-size imageDownload as PowerPoint slide