Enantioselective Thiourea‐Catalyzed Acyl‐Mannich Reactions of Isoquinolines

Abstract

Inexpensive aromatic feedstocks are substrates for highly enantioselective acylative Mannich reactions catalyzed by a thiourea chiral hydrogen-bond donor 1. This methodology provides access to useful 1-substituted dihydroisoquinolines (see scheme; TrocCl=2,2,2-trichloroethyl chloroformate, TBS=tert-butyldimethylsilyl), which serve as precursors to enantioenriched 1-substituted tetrahydroisoquinolines.