Medicinal Chemical Studies on Antiplasmin Drugs. V. 4-Aminomethylcyclohexanecarboxylic Acid Derivatives having a Methyl Group at C_2 or C_3
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概要
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Four isomers of 4-aminomethyl-2-methylcyclohexanecarboxylic acid (9) were synthesized from 4-cyano-o-toluic acid (2) or cis or trans 2-methyl-4-oxocyclohexanecarboxylic acid (5), and the isomers of 4-aminomethyl-3-methylcyclohexanecarboxylic acid (23) were also synthesized from 4-cyano-m-toluic acid (13) or ethyl cis or trans 7-methyl-1,4-dioxaspiro [4. 5] decane-8-carboxylate (15). The configurations of these isomers were determined on the basis of those of the starting materials and by leading them to dimethyl 2-methylcyclohexane-1,4-dicarboxylate (12), which was compared with 12 obtained from 5-methylbicyclo [2. 2. 2] oct-2-ene (10). The preferred conformations of the isomers in aqueous solution were deduced from the nuclear magnetic resonance spectra. The antiplasmin activity of t-4-aminomethyl-c-3-methyl-r-1-cyclohexanecarboxylic acid (23B), which is thought to exist in the 1-e, 3-e, 4-e form in aqueous solution, and which was the most active among the compounds tested in this study, was only about 0.64 times that of trans 4-aminomethylcyclohexanecarboxylic acid (1B).
- 公益社団法人日本薬学会の論文
- 1979-12-25
著者
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磯田 純郎
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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磯田 純郎
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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磯田 純郎
Research Institute Daiichi Seiyaku Co. Ltd.
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