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Updated: May 10, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Facile synthesis of 5-arylidene thiohydantoin by sequential sulfonylation/desulfination reaction
Jintao Han1, Hongbo Dong, Zhihong Xu
1Department of Applied Chemistry, China Agricultural University, Beijing 100193, China. wangma@cau.edu.cn.
Abstract:
The sequential sulfonylation/desulfination reactions of 5-benzylthiohydantoin with excess arylsulfonyl chlorides in the presence of triethylamine have been developed to afford a wide range of 5-arylidene thiohydantoin derivatives in moderate to excellent yields. A plausible sulfonylation/desulfination mechanism was proposed. The bioassay showed that these compounds exhibit certain fungicidal activities with the 71.9% inhibition rate of 2K against B. cinerea, and 57.6% inhibition rate of 2m against A. solani, respectively.
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