Readily Available Highly Active [Ti]-Adamantyl-BINOL Catalysts for the Enantioselective Alkylation of Aldehydes

[Image: see text] A series of enantiopure (R)-adamantyl 1,1′-binaphthalene-2,2′-diols were successfully synthesized in a straightforward one-step reaction from commercial products with excellent overall yields. The activity of chiral titanium catalyst derived from (R)-3,6,6′-tri(adamantan-1-yl)-[1,1′-binaphthalene]-2,2′-diol ligand, (R)-(2)-Ti, in the enantioselective asymmetric alkylation of aldehydes is significantly enhanced (up to 98% yield and 99% ee).