Highly Enantioselective One-Pot Synthesis of Chiral β-Heterosubstituted Alcohols via Ruthenium-Prolinamide-Catalyzed Asymmetric Transfer Hydrogenation

The utility of a chiral Ru-prolinamide catalytic system has been demonstrated in one-pot synthesis of optically active beta-triazolylethanol and beta-hydroxy sulfone derivatives. The said methodology proceeds through asymmetric transfer hydrogenation of in situ formed ketones of the corresponding chiral products. Various chiral prolinamide ligands were screened, and ligand L6 with isopropyl groups substituted at the ortho position has shown excellent activity at 60 degrees C in aqueous medium producing up to 95% yield and 99.9% enantioselectivity.