GAP Peptide Synthesis via Design of New GAP Protecting Group: An Fmoc/tBu Synthesis of Thymopentin Free from Polymers, Chromatography and Recrystallization.

GAP Peptide Synthesis via Design of New GAP Protecting Group: An Fmoc/tBu Synthesis of Thymopentin Free from Polymers, Chromatography and Recrystallization.
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DOI:
10.1002/ejoc.201600026
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发表时间:
2016-03
影响因子:
2.8
通讯作者:
Li G
Li G
中科院分区:
化学3区
文献类型:
--
作者:
Seifert CW;Paniagua A;White GA;Cai L;Li G

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报道了一种新的Fmoc/TBU固相多肽合成方法及新型苄基GAP保护基团的研制。这种新的间隙保护基团被用来代替聚合物载体,无需层析、重结晶或聚合物载体即可促进C→N Fmoc多肽的合成。GAP基团可以高产率地添加和移除,并用于合成1g以上的免疫刺激剂胸腺五肽,总收率(83%)和纯度(99%)都很高。
A novel method for Fmoc/tBu solution-phase peptide synthesis and the development of a new benzyl-type GAP protecting group is reported. This new GAP protecting group is utilized in place of a polymer support, facilitating C→N Fmoc peptide synthesis without chromatography, recrystallization, or polymer supports. The GAP group can be added and removed in high yield, and was used to synthesize over 1 gram of the immunostimulant, thymopentin, in high overall yield (83%) and purity (99%).