Convenient Entry to ¹⁸F-Labeled Amines through the Staudinger Reduction.

ABSTRACT: 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 ¹⁸F-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 ¹⁸F-labeled azides to primary amines by means of the Staudinger reduction. Aliphatic and aromatic ¹⁸F-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

SUBMITTER: Steen EJL 

PROVIDER: S-EPMC6471115 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature