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基于D-Pro-Gly构象限制性模块拟肽的合成 被引量:2

Synthesis of Conformationally Constrained Peptides Based on D-Pro-Gly Module
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摘要 设计了C-端和N-端二肽模块,通过液相合成法经DIC-HOBt缩合、混合酸酐缩合及脱保护等反应高效合成了含有构象限制性模块D-Pro-Gly内核、N-末端为伯胺、且能形成稳定β-转角结构的四肽系列化合物——H-Leu-D-Pro-Gly-Leu-OH,H-Leu-D-Pro-Gly-Val-OH和H-Leu-D-Pro-Gly-Val-OH,总收率分别为49.02%,40.13%和50.88%,其结构经1H NMR,13C NMR,ESI-MS和HR-MS确证。 The tetrapeptides containing a terminated primary amine and conformationally restricted DPro-Gly segment as a strongly β-turn-nucleating element,H-Leu-D-Pro-Gly-Leu-OH,H-Leu-D-ProGly-Val-OH and H-Leu-D-Pro-Gly-Val-OH,were designed and synthesized efficiently by condensation of N-module dipeptides with C-module dipeptides in solution. The total yield was 49. 02%, 40. 13% and 50. 88%,respectively. The structures were confirmed by1H NMR,13C NMR,ESI-MS and HR-MS.
出处 《合成化学》 CAS CSCD 北大核心 2014年第1期76-80,共5页 Chinese Journal of Synthetic Chemistry
基金 甘肃省科技创新服务平台建设计划(1001TTPA005,1103TTPA009)
关键词 C-端二肽模块 N-端二肽模块 D-Pro-Gly β-转角 全合成 C-module dipeptides N-module dipeptides D-Pro-Gly β-turn total synthesis
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