| Autor: |
Mizushima G; Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan., Fujita H; Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan., Kunishima M; Faculty of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical, and Health Sciences, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan.; Faculty of Pharmaceutical Sciences, Kobe Gakuin University, 1-1-3 Minatojima, Chuo-ku, Kobe, Hyogo 650-8586, Japan. |
| Abstrakt: |
A triazinyluronium-based dehydrative condensing reagent, 2-(4,6-dimethoxy-1,3,5-triazin-2-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate (DMT-TU), has been developed. Unlike commonly used guanidinium- and uronium-based reagents, DMT-TU does not contain high-energy N-N and N-O bonds, reducing its explosivity, as suggested by differential scanning calorimetry. Using DMT-TU in the presence of i Pr 2 EtN at room temperature, carboxylic acids and amines were effectively converted to their corresponding amides. Additionally, peptide bond formation with DMT-TU exhibited suppressed racemization ratios. |
