To directly produce an optically active α-substituted-β-aminoketone derivative from an optically inactive starting raw material by carrying out asymmetric Mannich reaction using a specific comples, a Lewis acid and a specific derivative.
(A) A synthetic zeolite, (B) a ketone and (C) an optically active aluminum-alkali metal-binaphthol complex of formula I, etc., are stirred and mixed in a solvent under an inert gas atmosphere and the mixture is reacted with (D) a Lewis acid of formula II (M is lanthanum, ytterbium or scandium; (m) is a positive number) and an α-aminoether derivative of formula III [R1 is a lower alkyl, phenyl or benzyl; R2 and R3 are each an (un)saturated lower alkyl or the like] to obtain the objective derivative of formula IV [R4 is a group of formula V (R7 is trifluoromethyl or a lower alkyl) 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
