Accessing the disallowed conformations of peptides employing amide-to-imidate modification.
نویسندگان
چکیده
Selective modification of the C-terminal amide in peptides to dihydrooxazine (a novel stable imidate isostere) by intramolecular nucleophilic cyclo-O-alkylation of the corresponding N-(3-bromopropyl)amides results in constraining of the C-terminal residue in natively disallowed conformations both in crystals and in solution.
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ورودعنوان ژورنال:
- Chemical communications
دوره 47 33 شماره
صفحات -
تاریخ انتشار 2011