Atroposelective [4+1] annulation for the synthesis of isotopic isoindolinones bearing both central and axial chirality

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O-labeled atropisomers featuring both central and axial chiralities are synthesized with high enantioselectivities and diastereoselectivities and good to excellent isotopic incorporation. Experimental and density functional theory studies suggest that the reaction involves a sequential condensation, cyclization and isomerization cascade, in which the second step is the enantio-determining process.