(2S,4R)-4-Methylglutamic acid, a high affinity (IC50 = 35 nM) and selective ligand for the kalnate (KA) receptor subtype, has been synthesized in multi-gram quantities starting from (S)- l-t-butoxycarbonyl-5-t-butyldiphenylsiloxymethylpyrrolidine-2-one. The diastereoselective methylation step provides the required trans product in 47% isolated yield.