Introduction of functional groups into peptides via N-alkylation |
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Authors: | Demmer O Dijkgraaf I Schottelius M Wester H-J Kessler H |
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Affiliation: | Department Chemie, Lehrstuhl II für organische Chemie, Technische Universit?t München, Lichtenbergstrasse 4, D-85747 Garching, Germany. |
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Abstract: | An optimized protocol for the mild and selective Fukuyama-Mitsunobu reaction was used for mono- and di- N-alkylation on solid support. Thereby, nonfunctionalized aliphatic and aromatic residues are quickly introduced into transiently protected, primary amines of a linear peptide. N-Alkylation can also be used to implement alkyl chains carrying (protected) functionalities suited for subsequent modification. Applicability of this method is demonstrated by various N-alkylated analogues of a cyclic CXCR4 receptor antagonist originally developed by Fujii et. al. |
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