To directly produce an optically active α-substituted-β-aminoketone derivative from an optically inactive starting raw material by the asymmetric Mannich reaction using an optically active lanthanum-alkali metal-binaphthol complex.
(A) A synthetic zeolite, (B) a ketone of formula II (R2 is a lower alkyl, benzyl, methoxy, phenyl, allyl, trifluoromethyl or a lower alkoxy- substituted alkyl or cyclopropylmetyl; R6 is trifluoromethyl or a lower alkyl), etc., (C) a formaldehyde derivative and (D) a secondary amine of formula III [R3 and R4 are each an (un)saturated lower alkyl or the like] are subjected to asymmetric Mannich reaction under an inert gas atmosphere in a solvent in the presence of (E) an optically active lanthanum-alkali metal-binaphthol complex of formula I (X is Li or Na), etc., to obtain the objective derivative of formula IV (R1 is a group of formula V or the like) having asymmetric structure induced at the α-position of the component B. The derivative has central muscle relaxing action.
IIDA TAKEHIKO
ARAI TAKAYOSHI
SHIBAZAKI MASAKATSU
