CDI (1,1′-Carbonyldiimidazole)

IC50: Not available.

The common method of peptide synthesis is not feasible for industry use due to its poor yields. CDI, a new peptide forming reagent, is applied recently as a more direct agent for the formation of acyl-imidazoles. [1]

In vitro: CDI can be prepared straightforwardly by the reaction of phosgene with four equivalents of imidazole under anhydrous conditions. It served as a convenient reagent for peptide synthesis since its side products, carbon dioxide and imidazole, were safe. Moreover, the carbon dioxide evolution was suggested to provide driving force for the peptide synthesis. A typical peptide-formation reaction was started by dissolving 0.010 mole acylamino acid in 10 ml tetrahydrofuran (THF), and after this, the evolution of carbon dioxide could be immediately observed. An hour later, the required amino acid or peptide ester was added with an amount of 0.010 molar. The reaction would be last for 15 min, but longer standing is probably beneficial. The formed peptide was then purified by wiping off the solvent under vacuum followed by washing the residue with acid, saturated bicarbonate and finally water.[1]

In vivo: So far, no in vivo data has been reported.

Clinical trial: So far, no clinical trial has been conducted.

Reference:
[1] Paul R, Anderson GW.  N,N'-Carbonyldiimidazole, a new peptide forming reagent. J. Am. Chem. Soc. 1960 Sep; 82: 4597-600.