Efficient palladium-catalyzed electrocarboxylation enables late-stage carbon isotope labelling.

ABSTRACT: Carbon isotope labelling of bioactive molecules is essential for accessing the pharmacokinetic and pharmacodynamic properties of new drug entities. Aryl carboxylic acids represent an important class of structural motifs ubiquitous in pharmaceutically active molecules and are ideal targets for the installation of a radioactive tag employing isotopically labelled CO₂. However, direct isotope incorporation via the reported catalytic reductive carboxylation (CRC) of aryl electrophiles relies on excess CO₂, which is incompatible with carbon-14 isotope incorporation. Furthermore, the application of some CRC reactions for late-stage carboxylation is limited because of the low tolerance of molecular complexity by the catalysts. Herein, we report the development of a practical

SUBMITTER: Batista GMF 

PROVIDER: S-EPMC10959938 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature