Optically active 4-aryl-2-pyrrolidne derivs. prepn. - from new phthalimido-butanoic acid ester(s) and hydrazine hydrate

摘要

Prepn. of (4S)- or (4R)-4-aryl-2-pyrrolidinone derivs. of formula (I) comprises reaction of optically active phthalimido-butanoic acid ester of formula (II) with hydrazine hydrate (III) and opt. removal of easily cleaved gps. and etherification of the resultant hydroxyl gps. In (I) and (II) R1= 1-7C hydrocarbyl opt. interrupted by oxygen; R2= 1-4C alkyl; R'1= R1 or an easily cleaved gp.; R3= 1-4C alkyl; Q= phthalimido. (II) are new cpds. USE/ADVANTAGE - (I) are useful as antiinflammatory agents, and treatment of neuroleptic and psychological disorders. The process is simple and gives high yields and high optical purity from accessible starting materials.