Enantioselective Pd-Catalysed Nucleophilic C(sp³)-H (Radio)fluorination.

ABSTRACT: Despite increasing demand for chiral fluorinated organic molecules, enantioselective C-H fluorination remains among the most challenging and sought-after transformations in organic synthesis. Furthermore, utilizing nucleophilic sources of fluorine is especially desirable for ¹⁸F-radiolabelling. To date, methods for enantioselective nucleophilic fluorination of inert C(sp³)-H bonds remain unknown. Herein, we report our design and development of a Pd-based catalytic system bearing bifunctional MPASA ligands which enabled highly regio- and enantioselective nucleophilic β-C(sp³)-H fluorination of synthetically important amides and lactams, commonly present in medicinal targets. The enantioenriched fluorinated products can be rapidly converted to corresponding c

SUBMITTER: Chekshin N 

PROVIDER: S-EPMC12393139 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature