SEQUENTIAL ALPHA-FUNCTIONALIZATION AND REDUCTIVE CYCLIZATION PROCESS: A FACILE ENANTISOSELECTIVE ENTRY TO CHIRAL 3-SUBSTITUTED TETRAHYDOQUINOLINE DERIVATIVES

摘要

This invention relates to a new and concise method for the construction of chiral 3-substituted tetrahydroquinoline derivatives based on L-proline catalyzed asymmetric a-functionalization of aldehyde, followed by reductive cyclization of nitro group under catalytic hydrogenation condition with high optical purities.