N-SUBSTITUTED AMINOMETHYL CYCLOPROPYL KETONE DERIVATIVE OR ITS SALT AND PRODUCTION METHOD USED FOR THEM

    公开(公告)号:JP2002322136A

    公开(公告)日:2002-11-08

    申请号:JP2001124499

    申请日:2001-04-23

    申请人: DAICEL CHEM

    摘要: PROBLEM TO BE SOLVED: To provide a new N-substituted aminomethyl cyclopropyl ketone derivative or its salt which are usable for obtaining an aminomethyl cyclopropyl ketone derivative, a 2-amino-1-cyclopropyl ethanol derivative or their salts. SOLUTION: The N-substituted aminomethyl cyclopropyl ketone derivative and its hydrohalide salt are represented by general formula (1). [wherein, R , R , and R are each independently H or an aliphatic hydrocarbon group; R and R are each independently H or an arylmethyl group which may have a substituent, C at the methyl position of the arylmethyl group combins with at least a H atom or a substitutable arylmethyl group, at least one of R and R is an arylmethyl group which may have a substituent].

    PRODUCTION OF OPTICALLY ACTIVE BETA-AMINOKETONES AND OPTICALLY ACTIVE PALLADIUM BINUCLEAR COMPLEX AND ITS PRODUCTION

    公开(公告)号:JPH11302236A

    公开(公告)日:1999-11-02

    申请号:JP20881998

    申请日:1998-07-24

    申请人: SAGAMI CHEM RES

    摘要: PROBLEM TO BE SOLVED: To efficiently synthesize the subject compounds useful as an intermediate for producing medicines, etc., by reacting a silyl enol ether with an imine in the presence of a specific catalyst. SOLUTION: A silyl enol ether represented by formula I [R is a substituted silyl; R is a (substituted) alkyl, a (substitute) alkenyl or the like; R and R are each H, a (substituted) alkyl, a (substituted) alkenyl or the like] is reacted with an imine represented by formula II [R is a (substituted) alkyl, a (substituted) alkenyl or the like; R is H, a (substituted) alkyl, a (substituted) alkenyl or the like] in the presence of a catalyst comprising a palladium- optically active phosphine ligand to afford the objective compounds represented by formula III. In the above reaction, e.g. N,N-dimethylformamide is preferably used as a solvent and the reaction is preferably carried out in the presence of a base such as calcium carbonate at a reactional temperature within the range of ambient temperature to 70 deg.C.