Effect of Brønsted Acids on the Activation of Mixed Anhydride/Mixed Carbonic Anhydride and C‐Terminal‐Free N‐Methylated Peptide Synthesis in a Micro‐Flow Reactor
Ting‐Ho Chen,
Akira Ando,
Otoka Shamoto
et al.
Abstract:Amidations employing mixed (carbonic) anhydrides have long been favoured in peptide synthesis because of their cost‐effectiveness and less waste generation. Despite their long history, no study has compared the effects of additives on the activation of mixed anhydrides and carbonic anhydrides. In this study, we investigated the amidation of mixed (carbonic) anhydride in the presence of a base and/or Brønsted acids. The use of NMI·HCl significantly improved the conversion of the mixed carbonic anhydride, while … Show more
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