ChemInform Abstract: External Chiral Ligand‐Induced Enantioselective Lithiation/S_E2 Reactions of Isochroman and Phthalan.

Abstract

External Chiral Ligand-Induced Enantioselective Lithiation/S E 2 Reactions of Isochroman and Phthalan.-Lithiation of isochroman and phthalan in the presence of a chiral bis(oxazoline) ligand followed by quenching with electrophiles results in asymmetric enantioselective formation of α-substituted derivatives. The method is applied to the preparation of the dopamine D 4 antagonist (R)-(VIII) (=U-101387).-(TOMOOKA, KAT-