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-basedlibrary; heterocyclic sp2–sp3 fragments; N-arylation; photoredox-nickel dual catalysis; Introduction
Heterocyclic sp2–sp3 fragments are
initiated a high-throughput program of fragment-basedlibrary generation and after shortcomings using more classical cross-coupling conditions, we turned our attention to the photoredox-nickel dual-catalysis strategy recently reported by MacMillan and Buchwald [10]. The reported conditions use lower
might come from ring opening [20][21].
Conclusion
In summary, we have developed a new workflow allowing to efficiently perform photoredox-nickel dual-catalyzed reactions in parallel for fragment-basedlibrary generation. We have screened 29 combinations of complex spirocyclic amines and (hetero)aryl