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Rigid Peptide Macrocycles from On‐Resin Glaser Stapling
ChemBioChem ( IF 3.2 ) Pub Date : 2018-04-26 , DOI: 10.1002/cbic.201800121
Philip A Cistrone 1 , Anthony P Silvestri 1 , Jordi C J Hintzen 1 , Philip E Dawson 1
Affiliation  

Set Glasers to staple! An intramolecular Glaser reaction employing copper chloride and an essential bpy‐diol ligand efficiently generated macrocyclic peptide diynes on solid support. The rigid and linear diyne bridge represents the most atom‐economical approach for i,i+4 and i,i+7 α‐helical stapling. Additionally, i,i+5,6 staples on disparate sides of the helix were shown to ablate α‐helicity.
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中文翻译:

树脂上格拉瑟钉合产生的刚性肽大环化合物

将格拉瑟斯装订起来!使用氯化铜和必需的 bpy-二醇配体的分子内格拉泽反应在固体载体上有效地生成大环肽二炔。刚性和线性二炔桥代表了ii +4 和ii +7 α 螺旋吻合的最原子经济方法。此外,螺旋不同侧的i , i +5,6 订书钉被证明可以消除 α 螺旋性。
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更新日期:2018-04-26
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