Synthesis of Enantiomerically Pure N-Substituted 4-Hydroxypyrrolidin-2-one Derivatives

摘要

Optically active 4-substituted pyrrolidin-2-one substructures can be found in various biologically active compounds such as CS-834,1,an oral carbapenem antibiotic drug,rolipram,2,an antidepressant agent and oxiracetame,3,a nootropic drug for the Alzheimer's disease.Chiral 4-hydroxypyrrolidin-2-one and its N-substituted derivatives are versatile intermediates for the synthesis of those compounds.Therefore,several methods for the synthesis of optically active 4-hydroxypyrrolidin-2-one derivatives have been developed including methods using enzymatic reaction and multistep synthsis from a chiral natural intermediate.