用于主链环化的新型甘氨酸构建单元：合成及掺入模型肽中。

Novel Gly building units for backbone cyclization: synthesis and incorporation into model peptides.

作者信息

Gazal Sharon, Gellerman Gary, Gilon Chaim

机构信息

Department of Organic Chemistry, Hebrew University of Jerusalem, Jerusalem 91904, Israel.

出版信息

Peptides. 2003 Dec;24(12):1847-52. doi: 10.1016/j.peptides.2003.09.020.

DOI:10.1016/j.peptides.2003.09.020

PMID:15127936

Abstract

We report the preparation of novel building units for backbone cyclization that have the general formula Fmoc-Nalpha[CH(R)CO2Al]Gly-OH. These building units were prepared by the reductive alkylation method using allyl esters of several amino acids as starting material and hence, respectively, contain the side chain of these amino acids. These N-alkylated Gly building units were incorporated in model backbone cyclic peptides. The resulting crude backbone cyclic peptides were obtained in high degree of purity according to HPLC and mass spectrometric analyses.

摘要

我们报道了用于主链环化的新型构建单元的制备，其通式为Fmoc-Nα[CH(R)CO₂Al]Gly-OH。这些构建单元通过还原烷基化方法制备，使用几种氨基酸的烯丙酯作为起始原料，因此分别含有这些氨基酸的侧链。这些N-烷基化的甘氨酸构建单元被纳入模型主链环肽中。根据高效液相色谱（HPLC）和质谱分析，所得粗品主链环肽具有高纯度。