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The dipicolylamino group as an efficient leaving group for amide bond formation via hexafluoroisopropyl ester

Organic and Biomolecular Chemistry, ISSN: 1477-0520, Vol: 22, Issue: 8, Page: 1699-1707
2024
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Peptide dipicolylamide was prepared by the solid-phase method. The amide was activated by Cu(ii) ions in hexafluoroisopropanol and converted to the corresponding active ester. It was condensed with the C-terminal segment to realize segment coupling. The method was successfully applied to the synthesis of an atrial natriuretic peptide and RNase T1.

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