Synthetic approaches towards [18F]fluoro-DOG1, a potential radiotracer for the imaging of gastrointestinal stromal tumors |
| |
| Authors: | Martin Prause Sabrina Niedermoser Ralf Schirrmacher Carmen Wängler Björn Wängler |
| |
| Institution: | 1. Molecular Imaging and Radiochemistry, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany;2. Department of Oncology, Division Oncological Imaging, University of Alberta, 11560 University Avenue, Edmonton, AB T6G 1Z2 Canada;3. Biomedical Imaging, Department of Clinical Radiology and Nuclear Medicine, Medical Faculty Mannheim of Heidelberg University, Theodor-Kutzer-Ufer 1-3, 68167 Mannheim, Germany |
| |
| Abstract: | Gastrointestinal stromal tumors (GIST) can currently only be identified by invasive biopsy sampling followed by immunohistochemical analysis. It would however be highly advantageous to have a radioligand able to bind the calcium-activated chloride channel DOG1, which is specific for GIST, and thus enable the sensitive, non-invasive and specific functional imaging of the disease by Positron Emission Tomography (PET). For this purpose, we developed different synthetic strategies towards a 4-phenylthiazole-2-amine-based labeling precursor that can be directly reacted with 18F-fluoride to yield a radiotracer intended to bind DOG1. Of these, a boronic acid pinacol ester radiolabeling precursor could be efficiently reacted with 18F in a one-step reaction, and the target radioligand 18F]fluoro-DOG1 be obtained in radiochemical yields of 34.0?±?11.1% within 85?min overall synthesis time. |
| |
| Keywords: | DOG1 Gastrointestinal stromal tumors Fluorine-18 Positron Emission Tomography (PET) |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
