General methods have been devised for the synthesis of lactam-constrained dipeptide analogues having five-, six-, and seven-membered rings. Three different paths from protected chiral a-amino acids to lactams involving intramolecular alkylation, intramolecular acylation, and insertion of a one carbon unit by condensation with formaldehyde have been utilized. The first two methods produce chiral products stereospecifically, but considerable ...
