Transition-Metal-Free Thioamination of Arynes Using Sulfenamides

• DOI: 10.1021/acs.orglett.8b03966
• Publication Date: 2019-01-16T14:21:17Z
• Authors: Rahul N. Gaykar; Subrata Bhattacha...; Akkattu T. Biju
• Keywords: Aryne

The insertion of arynes into the S-N σ-bond sulfenamides allowing synthesis o-sulfanylaniline derivatives with reasonable functional group compatibility is presented. aryne generated from 2-(trimethylsilyl)aryl triflates using CsF in DME was key for success this transition-metal-free thioamination reaction, which involves new C-N and C-S bond formations a single step under mild conditions. Moreover, synthetic potential method demonstrated by antidepressant drug vortioxetine.