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An Alkyne Rod to Constrain a Peptide Backbone in an Extended Conformation
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2018-08-21 , DOI: 10.1002/ejoc.201800979
Adam Přibylka 1 , Viktor Krchňák 1, 2
Affiliation  

A peptide backbone was locked in an extended conformation by the introduction of a dialkyne rod attached to amide nitrogens via one and/or two carbon spacers. Linear precursors were obtained by means of solid‐phase synthesis from commercially available building blocks. Subsequently, 13‐ to 15‐membered peptide macrocycles were obtained through Cu‐catalyzed cyclization in solution.
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中文翻译:

炔烃棒,以限制在扩展构象中的肽骨干。

通过引入经由一个和/或两个碳间隔基连接到酰胺氮上的二炔基棒,将肽主链锁定在延伸的构象中。线性前体是通过固相合成从市售的构建基块中获得的。随后,通过溶液中的铜催化环化获得了13至15元的肽大环。
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更新日期:2018-08-21
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