To obtain the subject derivative having physiological activities such as immunosuppressive and therapeutic actions on neuropathy by selectively hydrolyzing an aminomalonic diester derivative with an esterase and then carrying out the enantiodivergent reducing reaction of the resultant hydrolyzate.

An α-substituted-α-protected aminomalonic diester derivative represented by formula I [R1 is an α-substituent group (e.g. a 1-10C alky group such as methyl group); at least one of R2 and R3 is a protecting group of amino group (e.g. benzyloxycarbonyl) and the rest is H or an alcohol residue of an ester (e.g. a 1-6C alkyl such as ethyl)] is selectively hydrolyzed in the presence of an esterase (e.g. a porcine liver esterase) to afford an opotically active α- substituted-α-protected aminomalonic monoester derivative represented by formula II, which is then subjected to an enantiomeric reducing reaction with a reducing agent (e.g. sodium tetrahydroborate) to produce the objective derivative represented by formula III (R5 is same as R4 in formula I of H).