news | 2021-09-17
White oblong tablets lying on a table.

Iridium-catalyzed C-H methylation and d3-methylation of benzoic acids

In the pharmaceutical industry, lead compounds that modulate the progression of a disease need to be synthesized. Drugs are synthesized in typically 10-20 synthetic steps, which requires a lot of time and synthetic efforts.

Often, analogues to specific known drugs are good candidates for discovering new pharmaceuticals. Instead of embarking into de-novo syntheses for each drug analog, they may be synthesized via late-stage functionalization (LSF) of the parent drug. LSF consists of transforming a complex drug in a single step into its analogue insufficient yield. This is a challenging task, as the functionalization must occur selectively, despite the complexity of the molecule.

Together with AstraZeneca colleagues, the Mistra SafeChem group of Martín-Matute have reported an iridium-catalyzed LSF of several marketed drugs through selective methylation and D3-methylation (deuteriation). The analogues formed had increased metabolic stability compared to the parent drug.

The full name of the article is Ingress Iridium-catalyzed C−H methylation and d3-methylation of benzoic acids with application to late-stage functionalizations.

Read the article here. External link.