Department of Chemistry, Zhejiang University , Hangzhou 310027, China.
Org Lett. 2014 Nov 7;16(21):5644-7. doi: 10.1021/ol5027156. Epub 2014 Oct 17.
A copper-mediated C-S/N-S bond-forming reaction via C-H activation that uses elemental sulfur has been developed. The addition of TBAI was found to be crucial for the success of this transformation. The method is scalable, shows excellent functional group tolerance, and is compatible with heterocycle substrates, providing efficient and practical access to benzoisothiazolones. The direct diversification of the benzoisothiazolone products into a variety of sulfur-containing compounds is also demonstrated.
一种通过 C-H 活化利用元素硫实现的铜介导的 C-S/N-S 键形成反应已经被开发出来。研究发现，添加 TBAI 对于该转化的成功至关重要。该方法具有可扩展性，对官能团具有良好的耐受性，并且与杂环底物兼容，为苯并异噻唑酮类化合物提供了高效实用的合成方法。此外，还证明了苯并异噻唑酮产物可以直接多样化转化为各种含硫化合物。
