1. Prodrug Approach toward the Development of a PET Radioligand for Imaging the GluN2A Subunits of the NMDA Receptor
- Author
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Simon M. Ametamey, Stefan Gruber, Valérie Waser, and Zacharias Thiel
- Subjects
Fluorine Radioisotopes ,Molecular Structure ,010405 organic chemistry ,Chemistry ,Stereochemistry ,Organic Chemistry ,Quinoxalinedione ,Prodrug ,010402 general chemistry ,Cleavage (embryo) ,Receptors, N-Methyl-D-Aspartate ,01 natural sciences ,Biochemistry ,0104 chemical sciences ,chemistry.chemical_compound ,Positron-Emission Tomography ,Radioligand ,NMDA receptor ,Moiety ,Prodrugs ,Radiopharmaceuticals ,Physical and Theoretical Chemistry - Abstract
A straightforward synthesis of a fluorine-18-labeled prodrug of AFA233 is reported. The key step in the preparation of [18F]AFA233-prodrug is the selective deprotection of the tert-butyl protection groups of the quinoxalinedione moiety without cleavage of the tert-butyl-S-acyl-2-thioethyl protection groups on the phosphate esters. In addition, the preparation of the nonradioactive prodrug reference compound of AFA233 is reported. ISSN:1523-7060 ISSN:1523-7052
- Published
- 2021
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