| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for producing an arylaminopropanol of formula I enriched with its enantiomer. SOLUTION: This method for producing the arylaminopropanol comprises (a) converting a compound of formula (II) to a compound of formula (III) enriched with its enantiomer, or a compound of formula (IV) to a compound of formula (V) by using hydrogen, a compound transferring hydrogen or their mixture in the presence of a transition metal catalyst, (b) performing the reaction of an amine of formula (VI) with the compound of formula (III) enriched with the enantiomer in the case of using the compound (II) in the process (a) to obtain the compound of formula (V) enriched with the enantiomer and (c) reducing the compound (V) enriched with the enantiomer for coverting it to the compound (I) enriched with the enantiomer. It is possible to synthesize the compound (1) in a high total yield, a high enantiomer excess and a high purity and in an industrial scale. Formula (I): Ar-CH(OH)-CH<SB>2</SB>- CH<SB>2</SB>-NR<SP>1</SP>R<SP>2</SP>(wherein, Ar is a substituted or unsubstituted aryl; R<SP>1</SP>, R<SP>2</SP>are each independently each H, a 1-20C alkyl, a 4-14C aryl or a 5-15C arylalkyl, or together form a 3-12C alkylene), Formula (II): Ar-CO-CH<SB>2</SB>-COOR<SP>3</SP>, Formula (III): Ar-CH(OH)-CH<SB>2</SB>-COOR<SP>3</SP>, Formula (IV): Ar-CO- CH<SB>2</SB>-CONR<SP>1</SP>R<SP>2</SP>, Formula (V): Ar-CH(OH)-CH<SB>2</SB>-CONR<SP>1</SP>R<SP>2</SP>(wherein, R<SP>3</SP>is H, a 1-20C alkyl, a 4-24C aryl or a 5-15C arylalkyl), Formula (VI): HNR<SP>1</SP>R<SP>2</SP>. COPYRIGHT: (C)2004,JPO |
