Internal Peptide Late-Stage Diversification: Peptide-Isosteric Triazoles for Primary and Secondary C(sp3)-H Activation
Internal Peptide Late-Stage Diversification: Peptide-Isosteric Triazoles for Primary and Secondary C(sp3)-H Activation
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DOI：
10.1002/anie.201710136
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发表时间：
2018-01-02
影响因子：
16.6
通讯作者：
Ackermann, Lutz
中科院分区：
文献类型：
--
作者：
Bauer, Michaela;Wang, Wei;Ackermann, Lutz
二级C(sp(3))-H芳基化是通过钯催化以三唑作为肽键等排体完成的。这种方法的独特之处在于可以在末端肽上实现二级 C(sp(3))-H 功能化以及对内部肽位置进行前所未有的位置选择性 C(sp(3))-H 功能化，为模块化肽后期多样化奠定了基础。
Secondary C(sp(3))-H arylations were accomplished by palladium catalysis with triazoles as peptide bond isosteres. The unique power of this approach is highlighted by the possibility of achieving secondary C(sp(3))-H functionalizations on terminal peptides as well as the unprecedented positional-selective C(sp(3))-H functionalization of internal peptide positions, setting the stage for modular peptide late-stage diversification.