Han Jintao, Dong Hongbo, Xu Zhihong, Lei Jianping, Wang Mingan
Department of Applied Chemistry, China Agricultural University, Beijing 100193, China.
Int J Mol Sci. 2013 Jun 13;14(6):12484-95. doi: 10.3390/ijms140612484.
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.
已开发出5-苄硫基乙内酰脲在三乙胺存在下与过量芳基磺酰氯的顺序磺酰化/脱磺酰化反应，以中等至优异的产率得到多种5-亚芳基乙内酰脲衍生物。提出了一种合理的磺酰化/脱磺酰化机理。生物测定表明，这些化合物表现出一定的杀菌活性，其中2K对灰葡萄孢的抑制率为71.9%，2m对茄链格孢的抑制率为57.6%。
