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Synthesis of Functionalized Isoquinolone Derivatives via Rh(III)-Catalyzed [4+2]-Annulation of Benzamides with Internal Acetylene-Containing α-CF 3 -α-Amino Carboxylates.

Daria V VorobyevaDmitry A PetropavlovskikhIvan A GodovikovFedor M DolgushinSergey N Osipov
Published in: Molecules (Basel, Switzerland) (2022)
A convenient pathway to a new series of α-CF 3 -substituted α-amino acid derivatives bearing pharmacophore isoquinolone core in their backbone has been developed. The method is based on [4+2]-annulation of N- (pivaloyloxy) aryl amides with orthogonally protected internal acetylene-containing α-amino carboxylates under Rh(III)-catalysis. The target annulation products can be easily transformed into valuable isoquinoline derivatives via a successive aromatization/cross-coupling operation.
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