A general and efficient method for the synthesis of spiro-2, 5-diketopiperazines (spiro-DKPs) is described. Cyclization of Boc-protected dipeptides containing spiro-amino acids by microwave assisted heating in water furnished the corresponding spiro-DKPs. The spiro- amino acids were prepared by combining stereoselective alkylation reactions using the Schöllkopf methodology for amino acid construction with Grubbs ring-closing metathesis ( ...