Amide formation may be conducted with or without HOBt. Biotage®PS-Carbodiimide has been found to give superior results in comparison with N-Cyclohexylcarbodiimide-NI-Me PS resin and the quaternary carbodiimide resin P-EDC. In general, PS-Carbodiimide was found to synthesize amides in high yield and purity without evidence of residual amine or carboxylic acid. Unreacted carboxylic acid, normally used in excess relative to the amine, remains bound to the resin during workup. PS-Carbodiimide may also be used for the synthesis of pentafluorophenyl (PFP) activated esters and N-hydroxysuccinimidyl esters.
Synthesis of amides (top) and activated PFP esters (bottom) using Biotage® PS-Carbodiimide resin.
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