To efficiently and simply synthesize an optically active amidine by reacting an imide eater with an amine immobilized on solid granules in the presence of a mixture solution comprising a halogenated hydrocarbon, a base and a lower alcohol.
This method for producing an amidine comprises (1) chemically binding a protected amine derivative or a compound having a functional group capable of being converted into an amino group to a solid reaction carrier, (2) removing the protecting group from the amino group or converting the functional group capable of being converted into an amino group into the amino group, (3) treating the amine, such as an amino acid, held no the solid carrier with an imide ester acid adduct (preferably an imide lower alkyl ester) in the pressure of a mixture comprising a halogenated hydrocarbon, a base and a lower alcohol (especially preferably a mixture solution of methylene chloride, triethylamine and methanol), and (4) if necessary, subjecting the amidine derivative held on the solid carrier to a protecting group-removing reaction and further to a derivation reaction and subsequently releasing the obtained amidine from the solid carrier.
ITO SATOSHI
KOITO SEITA
NISHIOKA AKIRA
