Patent ID: 6531594
Filing Date: 2003-03-11
Classification: C07D,Y02P

Abstract:
A process for producing 1H-3-aminopyrrolidine or a protonic acid salt thereof, which comprises:(a) reacting an amino-protected aspartic anhydride of formula (1): wherein R represents a benzyloxycarbonyl group which may have one or more substituents on the benzene ring, with a primary amine represented by the formula Râ€²NH2 wherein Râ€² represents an aralkyl group which may have one or more substituents on the aromatic ring, to obtain a reaction product; (b) subjecting said reaction product to cyclodehydration to obtain a 1-aralkyl-3-(protected amino)pyrrolidine-2,5-dione compound of formula (2): wherein R has the same meaning as in formula (1) and Râ€² is as defined above; (c) replacing R with a hydrogen at the 3-position amino group of the compound of formula (2) to obtain a 1-aralkyl-3-aminopyrrolidine-2,5-dione compound of formula (3): wherein Râ€² has the same meaning as in formula (2); (d) reducing the carbonyl groups of the compound of formula (3) to obtain either a 1-aralkyl-3-aminopyrrolidine compound of formula (4): wherein Râ€² has the same meaning as in formula (2), or a salt thereof with a protonic acid; and (e) subjecting said compound of formula (4) or said salt thereof to hydrogenolysis to obtain 1H-3-aminopyrrolidine or a protonic acid salt thereof.