Direct catalytic stereoselective synthesis of C4' functionalized furanoside and nucleoside derivatives with a tetrasubstituted stereocenter

A direct catalytic stereoselective synthesis of C4’ functionalized furanoside and nucleoside derivatives with a tetrasubstituted stereocenter is disclosed. The amine‐catalyzed stereoselective α‐aminomethylation reactions on furanoside‐derived aldehyde derivatives gave the corresponding C4’ functionalized D‐ or L‐ribose derivatives in good to excellent yields (67 − 94%) with up to >20:1 dr.