Solid phase synthesis of 1-substituted pyroglutamates

Starting from a dipeptide containing the Bu-t ester of glutamic acid, disub stituted 2-pyrrolidinones were prepared in good yield and high purity. Cycl ization takes place using DPPA as activating reagent. Diversity was achieve d through reductive alkylation of the starting dipeptide and N-alkylation f ollowing the cyclization step. This approach has been used for the synthesi s of both individual compounds and mixture-based combinatorial libraries. ( C) 2000 Elsevier Science Ltd, All rights reserved.