Synthesis and Hypnotic Activities of 4-Thio Analogues of N^3-Substituted Uridines
スポンサーリンク
概要
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Reaction of tri-O-acetyluiidine (1) with benzyl bromide or 2-chloroacetophenone in the presence of K_2CO_3 gave the N^3-substituted analogues 2a, c.Condensation of 1 with (±)-1-phenylethanol or 3, 5-dimethylbenzyl alcohol using the Mitsunobu reaction also gave 2b, d in good yields. These compounds were allowed to react with Lawesson's reagent and were subsequently treated with ammonia to afford the 4-thiouracil derivatives 5a-d. Compounds 5a-c showed moderate hypnotic activity in mice. However, N^3-(3, 5-dimethyl)benzyl derivatives 3d, 5d were found to be almost inactive in this assay.
- 2001-09-01
著者
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YAMAMOTO IKUO
Department of Laboratory Medicine, Miyazaki Medical College
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Kimura Toshiyuki
Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University
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Yamamoto Ikuo
Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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Maruyama T
Institute Of Pharmacognosy Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Kimura Toshiyuki
Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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KOZAI Shigetada
Institute of Pharmacognosy, Faculty of Pharmaceutical Sciences, Tokushima Bunri University
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MARUYAMA Tokumi
Institute of Pharmacognosy, Faculty of Pharmaceutical Sciences, Tokushima Bunri University
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Maruyama Tokumi
Institute Of Pharmacognosy Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Kozai S
Institute Of Pharmacognosy Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Yamamoto Ikuo
Department Of Bioapplied Chemistry Faculty Of Engineering Osaka City University
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