Coupling of racemic N-protected amino acids with amino components by means of 2-chloro-4,6-dimethoxy-1,3,5-triazine (CDMT) in the presence of chiral tertiary amines such as strychnine, brucine, and sparteine proceeds enantioselectively, affording appropriate amides or dipeptides in 69-85% yield. The configuration of the preferred enantiomer and enantiomeric enrichment depend on the structures o...

A novel acetyl chloride-mediated cascade transformation involving three components (benzyl carbamate, ethyl glyoxylate and arene nucleophiles) is reported. Aryl orthogonally protected α-amino acids are obtained in a one pot cascade, using a mild AcOH-AcCl system, via a critical autocatalytic dehydration-activation step ensuring an original and efficient Friedel-Crafts orchestration.

N-(Protected α-aminoacyl)benzotriazoles are powerful acylating agents, and they are used frequently for preparing peptides and their mimetics and conjugates. The present paper describes the synthesis and characterization of a new benzyl {2-[(2-(1H-benzo[d][1,2,3]triazol-1-yl)-2-oxoethyl)amino]-2-oxoethyl} carbamate.