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Solid-Phase Synthesis of Oligopeptides Containing Sterically Hindered Amino Acids on Nonswellable Resin Using 3-Nitro-1,2,4-triazol-1-yl-tris(pyrrolidin-1-yl)phosphonium Hexafluorophosphate (PyNTP) as the Condensing Reagent
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2018-01-17 00:00:00 , DOI: 10.1021/acscombsci.7b00184
Rintaro Iwata Hara 1 , Yuta Mitsuhashi 1 , Keita Saito 2 , Yusuke Maeda 3 , Takeshi Wada 1
Affiliation  

Peptides are still difficult to synthesize when they contain sterically hindered amino acids, such as α,α-disubstituted amino acids and N-substituted amino acids. In this study, solid-phase syntheses of oligopeptides containing multiple α-aminoisobutyric acid (Aib) residues were performed in high yields by using a nonswellable resin as the solid-support and 3-nitro-1,2,4-triazol-1-yl-tris(pyrrolidin-1-yl)phosphonium hexafluorophosphate (PyNTP) as the condensing reagent.

中文翻译:

以3-硝基1,2,4-三唑-1-基-三(吡咯烷-1-基)六氟磷酸((PyNTP)为缩合剂在固溶性树脂上固相合成含位阻氨基酸的寡肽

当肽包含空间受阻氨基酸时,例如α,α-二取代氨基酸和N-取代氨基酸,仍难以合成。在这项研究中,通过使用不可溶胀的树脂作为固相载体和3-硝基-1,2,4-三唑-1-,以高产率进行了包含多个α-氨基异丁酸(Aib)残基的寡肽的固相合成。六氟磷酸基-三(吡咯烷-1-基)phosph(PyNTP)作为缩合剂。
更新日期:2018-01-17
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