Efficient Synthesis of α‑Quaternary α‑Hydroxy-β-amino Esters via Silyl Glyoxylate-Mediated Three-Component Reactions

An
efficient method has been developed for the enantioselective
synthesis of fully protected α-quaternary α-hydroxy-β-amino
esters via the coupling of three components: aryl Grignard reagents
(or methyllithium), silyl glyoxylate, and N-tert-butanesulfinyl imines. This protocol enables successive
formation of two C–C bonds and two adjacent chiral carbons
with high stereocontrol in a one-pot operation.