Abstract
N-(alpha,beta-Unsaturated acyl)-alpha-amino acids, amides and esters are structural motifs of many biologically active natural products. An alternate and advantageous approach for the synthesis of N-(alpha,beta-unsaturated acyl)-alpha-amino acid derivatives is developed via acylation of unprotected alpha-amino acids with stable crystalline N-(alpha,beta-unsaturated acyl)benzotriazole. The proposed methodology provides a new synthesis for compound (9) which is a precursor to a novel cytotoxic agent.