Introduction of functional groups into peptides via N-alkylation

被引：48

作者：

Demmer, O. ^{[1
]}

Dijkgraaf, I. ^{[2
]}

Schottelius, M. ^{[2
]}

Wester, H. -J. ^{[2
]}

Kessler, H. ^{[1
]}

机构：

[1] Tech Univ Munich, Dept Chem, Lehrstruhl Organ Chem 2, D-85747 Garching, Germany

[2] Tech Univ Munich, Klinikum Rechts Isar, Nukl Med Klin & Poliklin, D-81675 Munich, Germany

来源：

ORGANIC LETTERS | 2008年 / 10卷 / 10期

关键词：

D O I：

10.1021/ol800654n

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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.

引用

页码：2015 / 2018

页数：4

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