Photocatalyzed radiosynthesis of 11C‐phenylacetic acids

Abstract

Fast and straightforward incorporation of radionuclides into pharmaceutically relevant molecules is one of the main barriers to preclinical and clinical tracer research. Late‐stage direct incorporation of cyclotron‐produced [11C]CO2 to afford carbon‐11‐labeled radiopharmaceuticals has the potential to provide ready‐to‐inject positron emission tomography agents in less than an hour. The present work describes photocatalyzed carboxylation of alkylbenzene derivatives to afford 11C‐phenylacetic acids. Reaction conditions and scope are investigated followed by application of this methodology to the preparative radiosynthesis of [11C]fenoprofen, a nonsteroidal anti‐inflammatory drug.