Stereoselective synthesis of antifungal sulfoximines, novel triazoles, II

被引:0
|
作者
Kawanishi, H [1 ]
Morimoto, H [1 ]
Nakano, T [1 ]
Watanabe, T [1 ]
Oda, K [1 ]
Tsujihara, K [1 ]
机构
[1] Tanabe Seiyaku Co Ltd, Discovery Res Lab, Toda, Saitama 3358505, Japan
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中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Novel triazole derivatives with N-substituted sulfoximine moiety were synthesized and evaluated for antifungal activity. These compounds showed only significantly weak activity and the N-H sulfoximine moiety was extremely important for the activity. A more practical and effective stereoselective synthesis of N-H sulfoximine, (R)-S-2-[(2R,3R)-3-(2,4-difluorophenyl)-3-hydoroxy-4-(1H-1,2,4-triazol-1-yl)]butyl-S-methylsulfoximine (1), which was considered to be the most promising compound, has been developed.
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页码:181 / 189
页数:9
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