Stereoselective Synthesis of Indolines via Organocatalytic Thioester Enolate Addition Reactions

摘要: A straightforward stereoselective synthesis route to indolin-3-yl acetates has been developed using organocatalytic addition reactions of monothiomalonates ortho-bromo nitrostyrenes as the key step. The products this highly one-pot addition–deprotection–decarboxylation sequence were easily further converted target acetates, via an intramolecular Buchwald–Hartwig coupling reaction. provided bearing tertiary and exocyclic quarternary stereogenic centers in excellent stereoselectivities overall yields 34–83%.