Sulfur-Mediated Aminothiolation of Terminal Alkynes: Regioselective Synthesis of Z -Trisubstituted Vinyl Sulfides

作者：Long‐Yong Xie, Ziyu Wang, Lu-Can Cheng, Jian Wen · 发表于：Organic Letters · 年份：2025 · DOI：10.1021/acs.orglett.5c01475 · 被引用次数：20 · 研究领域：Sulfur-Based Synthesis Techniques、Chemical Synthesis and Reactions、Synthesis and Catalytic Reactions

The first sulfur-mediated aminothiolation of terminal alkynes through a one-pot procedure under mild conditions has been established. This method is practical, easy to manipulate, and exhibits a wide substrate range with good functional group tolerance, resulting in Z -selective trisubstituted vinyl sulfides in moderate to high yields. The synthetic utility of this protocol is further highlighted by its applicability in scale-up reactions and late-stage modification of target products and drug molecules, making it a valuable tool for drug discovery. A mechanistic rationale is further supported by control experiments and DFT calculations.