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Copper‐Mediated Thiolation of Unactivated Heteroaryl C−H Bonds with Disulfides under Ligand‐ and Metal‐Oxidant‐Free Conditions
Advanced Synthesis & Catalysis ( IF 5.4 ) Pub Date : 2017-09-28 , DOI: 10.1002/adsc.201700949
Ya Li 1 , Yue-Jin Liu 1 , Bing-Feng Shi 1, 2
Affiliation  

Various sulfenylated heteroarenes were synthesized by a copper‐mediated C−H thiolation, which was assisted by a 2‐(pyridin‐2‐yl)isopropylamine (PIP‐amine) directing group. The reaction features a broad substrate scope, good functional group tolerance, ligand‐ and metal‐oxidant‐free conditions, exceptional compatibility with aliphatic disulfides, and excellent yields, providing a highly efficient approach to the biologically important sulfenylated heteroarenes.

中文翻译:

在无配体和无金属氧化剂的条件下,铜介导的未活化杂芳基CH键与二硫键的硫杂化

通过铜介导的CH巯基化反应合成了各种亚磺化杂芳基,并辅以2-(吡啶-2-基)异丙胺(PIP-胺)导向基团。该反应具有广泛的底物范围,良好的官能团耐受性,无配体和金属氧化剂的条件,与脂肪族二硫化物的优异相容性以及优异的收率,为生物学上重要的亚磺化杂芳烃提供了一种高效方法。
更新日期:2017-09-28
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