Broad Scope and High-Yield Access to Unsymmetrical Acyclic [¹¹ C]Ureas for Biomedical Imaging from [¹¹ C]Carbonyl Difluoride.

ABSTRACT: Effective methods are needed for labelling acyclic ureas with carbon-11 (t_1/2 =20.4 min) as potential radiotracers for biomedical imaging with positron emission tomography (PET). Herein, we describe the rapid and high-yield syntheses of unsymmetrical acyclic [¹¹ C]ureas under mild conditions (room temperature and within 7 min) using no-carrier-added [¹¹ C]carbonyl difluoride with aliphatic and aryl amines. This methodology is compatible with diverse functionality (e. g., hydroxy, carboxyl, amino, amido, or pyridyl) in the substrate amines. The labelling process proceeds through putative [¹¹ C]carbamoyl fluorides and for primary amines through isolable [¹¹ C]isocyanate intermediates. Unsymmetrical [¹¹ C]ureas are produced wit

SUBMITTER: Jakobsson JE 

PROVIDER: S-EPMC10134011 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature