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Described herein is the enantioselective syntheses of (+)‐ and (−)‐rishirilide B from the corresponding optically active β‐substituted tetralones, which were obtained by oxidative kinetic resolution based on α‐hydroxylation in the presence of a chiral guanidine‐bisurea bifunctional organocatalyst. Benzylic oxidation of the tetralones at C1 followed by regioselective isomerization of the oxabenzonorbornadiene...
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