Synthesis of enantioenriched spirocyclic 2-arylpiperidines via kinetic resolution

Org Biomol Chem. 2024 Feb 21;22(8):1602-1607. doi: 10.1039/d4ob00011k.

Abstract

Kinetic resolution of N-Boc-spirocyclic 2-arylpiperidines with spiro substitution at C-4 was achieved with high enantiomeric ratios using the chiral base n-BuLi/sparteine. Cyclopropanation or metallaphotoredox catalysis were used to access the piperidines, which could be further functionalised without loss of enantiopurity, highlighting their use as potential 3D fragments for drug discovery.