Photocatalytic α‐Tertiary Amine Synthesis via C−H Alkylation of Unmasked Primary Amines

• Alison S. H. Ryder¹ William B. Cunningham²
• George Ballantyne²
• Tom Mules²
• Anna G. Kinsella²
• Jacob Turner-Dore²
• Catherine M. Alder³
• Lee J. Edwards³
• Blandine S. J. McKay³
• Matthew N. Grayson²
• Alexander J. Cresswell²

• ¹Centre for Sustainable Chemical Technologies, University of Bath 1 South, Claverton Down, Bath, BA2 7AY (UK)
• ²Department of Chemistry, University of Bath 1 South, Claverton Down, Bath, BA2 7AY (UK) E-Mail: [email protected]
• ³Medicines Design, GSK Medicines Research Centre Gunnels Wood Rd, Stevenage, SG1 2NY (UK)

Catalytic strategies for the α‐C−H functionalisation of primary amines are a major challenge in organic synthesis. A photocatalytic protocol for the α‐C−H alkylation of unprotected primary amines that is amenable to the direct synthesis of α‐tertiary primary amines is reported. This process is readily scalable in continuous flow to provide access to decagram quantities of valuable γ‐lactams and azaspirocycles, for application in drug discovery.

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