Accelerating fragment-based library generation by coupling high-performance photoreactors with benchtop analysis

• Quentin Lefebvre,
• Christophe Salomé and
• Thomas C. Fessard

Beilstein J. Org. Chem. 2020, 16, 982–988, doi:10.3762/bjoc.16.87

• thus be rapidly accessed, identifying privileged or challenging scaffolds and paving the way for further exploration. Keywords: benchtop analytics; fragment-based library; heterocyclic sp2–sp3 fragments; N-arylation; photoredox-nickel dual catalysis; Introduction Heterocyclic sp2–sp3 fragments are

• often exhibit different reactivity from unstrained substrates [8]. N-Arylation of spirocyclic amines would be a very efficient strategy for the modular synthesis of heterocyclic sp2–sp3 fragments, but their lack of stability to strongly basic conditions and heating might be an issue in palladium

• , 29 combinations of bicycloalkylamines or spirocyclic amines with (hetero)aryl bromides were probed using this workflow, and the results are depicted in Scheme 2 and Scheme 3. To provide attractive heterocyclic sp2–sp3 fragments, we mainly focused on coupling 3-bromopyridine to five different classes