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Synthesis
DOI: 10.1055/a-2802-6034
DOI: 10.1055/a-2802-6034
Paper
Synthesis of 4-Sulfenyl-Isocoumarins via Thio-Annulation of 2-Alkynyl-benzonate with RSCl: In Situ Preparation using Disulfides and HCl/HNO3
Authors
Funding Information This project was financially supported by the National Natural Science Foundation of China (No. 21602036), the Guangxi Natural Science Foundation (Grant No. 2025GXNSFHA069092).

Abstract
We have developed a novel and metal-free method to construct the derivatives of 4-sulfenyl isocoumarins via thio-annulation of 2-alkynyl benzoates with sulfenyl chlorides which is in situ prepared by disulfides and HCl/HNO3. The reaction shows high functional group tolerance and can be scaled up to the gram-scale with less loss in yield. Both sulfide groups of the disulfide reagent were used in the reaction.
Publication History
Received: 31 December 2025
Accepted after revision: 02 February 2026
Accepted Manuscript online:
02 February 2026
Article published online:
11 February 2026
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