Scientific Literature

Primary α-tertiary amine synthesis via α-C–H functionalization

Abstract A quinone-mediated general synthetic platform for the construction of primary α-tertiary amines from abundant primary α-branched amine starting materials is described. This procedure pivots on the efficient in situ generation of reactive ketimine...

Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines

Abstract In fragment-based drug discovery (FBDD), a weakly binding fragment hit is elaborated into a potent ligand by bespoke functionalization along specific directions (growth vectors) from the fragment core in order to complement the 3D structure of the target...

Photocatalytic Three-Component Umpolung Synthesis of 1,3-Diamines

Abstract A visible-light-mediated photocatalytic umpolung synthesis of 1,3-diamines from in situ-generated imines and dehydroalanine derivatives is described. Pivoting on a key nucleophilic addition of photocatalytically generated α-amino radicals to...

Late-Stage Sulfoximidation of Electron-Rich Arenes by Photoredox Catalysis

Abstract The sulfoximine group has been reported as a versatile and beneficial functionality for pharmaceutical or agrochemical entities. Herein, we report the Csp2–H sulfoximidation of electron-rich arenes ­under the irradiation of blue light using an organic...