Medicinal Chemical Studies on Antiplasmin Drugs. VII. Oxa Analogs of 4-Aminomethylcyclohexanecarboxylic Acid
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概要
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The two isomers of 5-aminomethyltetrahydro-2H-pyran-2-carboxylic acid (9) and those of 5-aminomethyl-1,4-dioxane-2-carboxylic acid (18) were synthesized from 2-ethoxycarbonyl-3,4-dihydro-2H-pyran-5-carboxylic acid chloride (2) and dimethyl 1,4-dioxane-2,5-dicarboxylate (15), respectively. From the aminoacetal (19) and dimethyl bis (hydroxymethyl) malonate (21), trans-2-aminomethyl-1,3-dioxane-5-carboxylic acid (26A) was synthesized. The configurations of these isomers were determined on the basis of their nuclear magnetic resonance spectra, and the preferred conformations of the isomers in aqueous solution were similarly deduced. No compound showed antiplasmin activity more potent than that of trans-4-aminomethylcyclohexanecarboxylic acid (1A).
- 公益社団法人日本薬学会の論文
- 1980-08-25
著者
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山口 等
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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磯田 純郎
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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佐藤 嘉生
Research Institute, Daiichi Seiyaku Co., Ltd.
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山口 等
Research Institute Daiichi Pharmaceutical Co. Ltd.
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磯田 純郎
Research Institute Daiichi Seiyaku Co. Ltd.
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佐藤 嘉生
Research Institute Daiichi Seiyaku Co. Ltd.
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平田 三四司
Research Institute, Daiichi Seiyaku Co., Ltd.
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平田 三四司
Research Institute Daiichi Seiyaku Co. Ltd.
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