Access to Thienopyridine and Thienoquinoline Derivatives via Site-Selective C–H Bond Functionalization and Annulation

作者：Runfa He, Yang Liu, Yingqi Feng, Lu Chen, Yubing Huang, Feng Xie, Yibiao Li · 发表于：Organic Letters · 年份：2022 · DOI：10.1021/acs.orglett.2c00903 · 被引用次数：23 · 研究领域：Catalytic C–H Functionalization Methods、Sulfur-Based Synthesis Techniques、Synthesis and Catalytic Reactions

To develop of an effective synthetic methodology for biologically relevant thienopyridines, a concise and efficient protocol is described for the synthesis of a series of substituted thienopyridine and thienoquinoline derivatives with high selectivity using EtOCS 2 K as the sulfur source. The reaction proceeds via metal-free, site-selective C–H bond thiolation and cyclization of the alkynylpyridine and alkynylquinoline substrates.