Spirocyclic tetrahydronaphthyridines (THNs) are valuable structural motifs in medicinal chemistry, but the modular and scalable synthesis of this specific motif remains challenging. Here, the authors develop an automated and continuous flow synthesis of 1,8-THN and 1,6-THN analogues based on photoredox-catalysed hydroaminoalkylation, demonstrating the concise synthesis of the spirocyclic THN core of Pfizer’s MC4R antagonist PF-07258669.
- Qiao Cao
- Joshua D. Tibbetts
- Alexander J. Cresswell
