Convenient Entry to (18)F‐Labeled Amines through the Staudinger Reduction

Fluorine‐18 possesses outstanding decay characteristics for positron emission tomography (PET) imaging. Therefore, it is ideally suited for clinical applications. As such, improved strategies to incorporate fluorine‐18 into bioactive molecules are of utmost importance. Indirect (18)F‐labeling with amino‐functionalized synthons is a convenient and versatile approach to synthesize a broad variety of PET tracers. Herein, we report a method to convert (18)F‐labeled azides to primary amines by means of the Staudinger reduction. Aliphatic and aromatic (18)F‐labeled azides were converted into the corresponding amines with high conversion yields. The method was easily automated. From a broader perspective, the applied strategy results in two useful synthons from a single precursor and thus increases the flexibility to label diverse chemical scaffolds with minimal synthetic effort.