C(sp3)-H arylation to construct all-syn cyclobutane-based heterobicyclic systems: a novel fragment collection.

摘要: All-syn fused cyclobutanes remain an elusive chemotype and thus present interesting synthetic challenge. Herein, we report the successful application of Pd-catalysed C(sp3)-H arylation cyclobutane compounds to generate all-syn heterobicyclic fragments using innovative 'inside-out' approach. Through this strategy a virtual collection 90 fragments, which demonstrate have enhanced three-dimensionality superior fragment-like properties compared existing collections.