Synfacts 2023; 19(04): 0424
DOI: 10.1055/s-0042-1752640
Peptide Chemistry

Synthesis of N-Formyl Amino Acid Esters

Contributor(s):
Hisashi Yamamoto
,
Isai Ramakrishna
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.
 

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.


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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.


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Publication History

Article published online:
17 March 2023

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