Neurotropic and Psychotropic Agents. IV. Synthesis and Pharmacological Properties of 7-Chloro-5-(2-chlorophenyl)-2-(2-dimethylaminoethylthio)-3H-1,4-benzodiazepine and Related Compounds
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概要
- 論文の詳細を見る
The synthesis and pharmacological properties of 7-chloro-5-(2-chlorophenyl)-2-(2-dimethylaminoethylthio)-3H-1,4-benzodiazepine (III-1) and related compounds are described. Compound III-1 was prepared from the thiolactam (II-1) by treatment with 2-dimethylaminoethyl chloride in the presence of base in aqueous methanol and 7-chloro-5-(2-ohlorophenyl)-2-methoxy-3H-1,4-benzodiazepine (IV) was obtained as a by-product. The latter (IV) was hydrolyzed in acid medium to give methyl (E)-[2-amino-5-chloro-α-(2-chlorophenyl) benzylidene] aminoacetate (syn-form) (XIX), which was converted into the 1,4-benzodiazepine (I-1) by further acid treatment. Compound XIX isomerized to the corresponding anti-form (XXII) on heating. Most of the compounds prepared had an effect similar to that of diazepam in causing taming and anticonvulsant effects in mice.
- 社団法人日本薬学会の論文
- 1982-04-25
著者
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松尾 昌昭
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.,
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植田 育男
Institute Of Scientific And Industrial Reseach Osaka University
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植田 育男
Central Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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谷口 清
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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松尾 昌昭
Central Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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谷口 清
Central Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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松尾 昌昭
New Drug Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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