Highly Enantio‐ and Diastereoselective L‐Proline Derived Acetylglucose Amide Catalyzed Aldol Reaction of Ketones to Aldehydes under Solvent‐Free Conditions.

A novel organocatalyst was developed from d -glucosamine and l -proline, which was shown to catalyze the direct aldol reaction of ketones with aldehydes in a highly diastereoselective and enantioselective manner under solvent-free conditions. The presence of 10 mol% catalyst could promote the reaction effectively, affording the desired aldol products in high yields (70–99%) and excellent selectivities (up to >99:1 dr and up to >99% ee).