Synthesis of Radiopharmaceuticals <i>via</i> "In-Loop" ¹¹C-Carbonylation as Exemplified by the Radiolabeling of Inhibitors of Bruton's Tyrosine Kinase.

ABSTRACT: Positron emission tomography (PET) is an important non-invasive tool to help guide the drug discovery and development process. Positron-emitting-radiolabeled drug candidates represent an important tool for drug hunters to gain insight into a drug's biodistribution and target engagement of exploratory biologic targets of interest. Recently, there have been several drug candidates that incorporate an acryloyl functional group due to their ability to form a covalent bond within the biological target of interest through Michael addition. Methods to incorporate a carbon-11 radionuclide into acrylamide derivatives remain challenging given the reactive nature of this moiety. Herein, we report the improved radiosynthesis of carbon-11-containing acrylamide drug candidates, [¹¹C]ibrutinib

SUBMITTER: Donnelly DJ 

PROVIDER: S-EPMC11440948 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature