1H-Fluoren-9-ylmethyl Chloroformate as a Coupling Reagent for Peptide Synthesis

Key words

coupling agents - Fmoc chloroformate - mixed anhydrides - peptide synthesis

Significance

The development of a rapid, racemization-free, practically simple, and cost-effective methods for the synthesis of peptides is an important process in peptide drug discovery. In 2003, Sureshbabu and co-workers developed 1H-fluoren-9-ylmethyl chloroformate (Fmoc-Cl) as an effective coupling reagent for the synthesis of peptides.

Comment

N-Protected amino acids smoothly reacted with a series of amino acid esters to provide various peptides in good yields with the help of Fmoc-Cl as a coupling reagent. This method is practically simple, rapid, and racemization-free; moreover, Fmoc-Cl is a commercially available, crystalline, bench-stable solid.