Metal-Free Selective Modification of Secondary Amides: Application in Late-Stage Diversification of Peptides
Metal-Free Selective Modification of Secondary Amides: Application in Late-Stage Diversification of Peptides
复制标题
仲酰胺的无金属选择性修饰：在多肽后期多样化中的应用
DOI：
10.1021/acs.orglett.1c01622
复制
发表时间：
2021-07-12
期刊：
影响因子：
5.2
通讯作者：
Raj, Monika
中科院分区：
文献类型：
--
作者：
Adebomi, Victor;Sriram, Mahesh;Raj, Monika
在这里，我们解决了一个长期存在的挑战，仲酰胺的位点选择性修饰，并提出了一个简单的两步，无金属的方法来选择性地修改一个特定的仲酰胺分子中含有多个伯和仲酰胺。密度泛函理论（DFT）提供了深入了解C-N键的活化。这项研究包括肽的后期修饰的独特化学进展，从而利用酰胺将各种官能团掺入天然和合成分子中。
Here we solve a long-standing challenge of the site-selective modification of secondary amides and present a simple two-step, metal-free approach to selectively modify a particular secondary amide in molecules containing multiple primary and secondary amides. Density functional theory (DFT) provides insight into the activation of C-N bonds. This study encompasses distinct chemical advances for late-stage modification of peptides thus harnessing the amides for the incorporation of various functional groups into natural and synthetic molecules.