STEREOSELECTIVE PRODUCTION OF DIHYDRO-QUINOLINE DERIVATIVE AND DIHYDROISOQUINOLINE DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To provide a stereoselective production process that can stereoselectively produce dihydroquinoline derivatives and dihydroisoquinoline derivatives with high optical purity. SOLUTION: In this stereoselective production process for dihydroquinoline derivative or dihydroisoquinoline derivative, quinoline or isoquinoline represented by formula I or formula II (wherein R1 and R2 are each H, an alkyl, an alkoxy, an aralkyl, a halogen or they may form dialkylamino or alkylenedioxy; R3 is H or an alkyl) is allowed react with an acid halide represented by R4COX of formula V [wherein R4 is a (substituted) alkyl, a (substituted) alkenyl, a cycloalkyl, a (substituted) aryl, a (substituted) aralkyl, a (substituted) aromatic heterocyclic ring, an alkoxy, an aryloxy, aralkyloxy or a dialkylamino; X is Cl or Br] in the presence of a cyanidation agent and an asymmetric catalyst represented by formula VI [Q is a (substituted) phenyl or alkyl].