We have discovered a versatile and economical synthesis for the preparation of a large variety of homochiral compounds in which a heterocyclic ring system is fused to the β-carbon atom of L-alanine. This methodology has recently been extended to encompass the preparation of analogues of the lower homologue, ibotenic acid. The synthesis, shown in Scheme 1, involves reaction of bisnucleophiles with an aldehyde of a pyroglutamic acid derivative 3 (n = 1) or an aldehyde of a β-lactam 3 (n = 0) or with their homologues 11.