Patent ID: 7186865

Claim:
A process for producing an optically active 1-(fluoro-, trifluoromethyl- or trifluoromethoxy-substituted phenyl)alkylamine N-monoalkyl derivative represented by the formula 4, the process comprising the steps of: (a) reacting an optically active secondary amine, represented by the formula 1, with an alkylation agent represented by the formula 2, in the presence of a base, thereby converting the secondary amine into an optically active tertiary amine represented by the formula 3; and (b) subjecting the tertiary amine to a hydrogenolysis, thereby producing the N-monoalkyl derivative, wherein R represents a fluorine atom, trifluoromethyl group or trifluoromethoxy group, n represents an integer of from 1 to 5, R 1 represents an alkyl group having a carbon atom number of from 1 to 6, Me represents a methyl group, Ar represents a phenyl group or 1- or 2-naphthyl group, and * represents a chiral carbon, R 2 —X [2] wherein R 2 represents an alkyl group having a carbon atom number of from 1 to 6, and X represents a leaving group, wherein R, n, R 1 , Me, Ar, and * are defined as in the formula 1, and R 2 is defined as in the formula 2, wherein R, n, R 1 , and * are defined as in the formula 1, and R 2 is defined as in the formula 2.