Radiosyntheses of two positron emission tomography probes: [11C]Oseltamivir and its active metabolite [11C]Ro 64-0802

Oseltamivir phosphate (Tamiflu®, 1·H3PO4 is an orally active anti-influenza drug, which is hydrolyzed by esterase to its carboxylate metabolite Ro 64-0802 (2) with potent activity inhibiting neuraminidase. In this study, for the first time, we synthesized carbon-11-labeled oseltamivir ([11C]1) and Ro 64-0802 ([11C]2) as two novel positron emission tomography probes and demonstrated that [11C]1 had twofold higher radioactivity concentration in the mouse brains than [11C]2.

Graphical abstractRadiosyntheses of [11C]oseltamivir and its active metabolite [11C]Ro 64-0802 as two positron emission tomography probes and their radioactivity concentrations in the mouse brains are reported for the first time.Figure optionsDownload full-size imageDownload as PowerPoint slide