The Design and Synthesis of [18F]Fluoride-trap Prosthetic Groups for Potential Applications in PET Imaging.

摘要

Positron emission tomography (PET) has become a key component to the detection of many diseases, including cancer. In order to discover and monitor these diseases by PET, imaging probes (radiotracers) are required. Incorporation of the radioisotope (e.g. Fluorine-18) is frequently done using a specific linker (prosthetic group).;The synthesis of two novel [18F]fluoride-trap prosthetic groups for application as radiotracers in PET, based on silicon- and boron-fluoride binding, was accomplished. A bifunctional boronate ester was designed for radiolabeling with [18F]fluoride and incorporation into the radiotracer by "click" chemistry. The prosthetic group was successfully labeled with a 55% [18F]fluorine-incorporation. Efforts to label the aryltetrafluorosilicate precursor with either 19F or 18F were, however, not successful.