Giard T,
*,
Bénard D,
Plaquevent J.-C.
Laboratoire des Fonctions Azotées et Oxygénées Complexes de l'IRCOF, Mont Saint Aignan, France
A Mild Method for Formylating Amino Esters Without Using any Formylating Agent.
Synthesis 1998; 297-300
DOI:
10.1055/s-1998-2025
Key words
formylation - amino acid esters - oxaziridines
Significance
N-Formyl amino acids and peptides play a crucial role in peptide drug discovery. Thus, synthetic chemists are in search of mild and simple methods for the synthesis of N-formyl amino acids. In 1998, Giard and co-workers developed a simple method for the synthesis of N-formyl amino acid esters without using formylating agents.
Comment
A series of N-formyl amino acid esters were synthesized in three steps with excellent yields without using any formylating agent. This protocol is practically simple, mild, and proceeds without racemization.
