首页|Enantioselective Arylation of Tetrasubstituted Enamines: Access to Enantioenriched Indolenine and 1H-Indole Derivatives
Enantioselective Arylation of Tetrasubstituted Enamines: Access to Enantioenriched Indolenine and 1H-Indole Derivatives
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NSTL
Amer Chemical Soc
Palladium-catalyzed intramolecular enantioselective <i>β- arylation of tetrasubstituted endocyclic and exocyclic enamines is developed. A range of optically active medium-ring fused indolenines or 3,3′-spiroindolenines were achieved in enantiomeric ratios up to 98:2 with Cs_(2)CO_(3) or K_(3)PO_(4) as the base in the presence of chiral PHOX ligands. The use of Ag_(3)PO_(4) as a base led to enantioenriched 1H-indoles in good enantiomeric ratios (up to 89:11) with (<i>S )-DIFLUORPHOS as a chiral ligand, which proceeded via a possible domino enamine-isomerization/<i>β- arylation sequence.
NSTL
Amer Chemical Soc
