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Vorobyeva, Daria V.; Petropavlovskikh, Dmitry A.; Godovikov, Ivan A.; Dolgushin, Fedor M.; Osipov, Sergey N.
Molecules (Basel, Switzerland), 12/2022, Volume: 27, Issue: 23Journal Article
A convenient pathway to a new series of α-CF3-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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