Synthesis of 2,3-Dihydro-1,4-benzodioxin Derivatives. II. : 5(or 6)-Acyl 2,3-Dihydro-1,4-benzodioxin Derivatives : New Phenoxyacetic Acid Diuretics
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概要
- 論文の詳細を見る
5(and 6)-Acyl-7,8-dichloro-2,3-dihydro-1,4-benzodioxin-2-carboxylic acids (VI) and related compounds were synthesized and tested for diuretic and antihypertensive properties. These compounds (VI) were prepared by the reaction of 3,4-dichloro-1,2-dihydroxybenzene (2) with epibromohydrin (EBH) in the presence of a base and the Friedel-Crafts acylation, or by acylation of 2 and reaction with EBH, followed by oxidation. Acylation of 7,8-dichlorodihydrobenzodioxin-2-ylmethanol (15a) gave the corresponding 5- and 6-acyl compounds, (17 and 10). Diuretic activity was generally observed when a 5-acyl substituent was present in the molecule. Compound 20e showed strong diuretic and antihypertensive activities, like indacrinone (II).
- 公益社団法人日本薬学会の論文
- 1988-09-25
著者
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林 邦雄
Shionogi Research Laboratories Shionogi & Co. Ltd.
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中村 益久
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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板崎 弘
Shionogi Research Laboratory, Shionogi & Co., Ltd.
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中村 益久
Shionogi Research Laboratories Shionogi & Co. Ltd.
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松浦 宗教
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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米谷 行男
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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松浦 宗教
Shionogi Research Laboratories Shionogi & Co. Ltd.
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米谷 行男
Shionogi Research Laboratories Shionogi & Co. Ltd.
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板崎 弘
Shionogi Research Laboratories Shionogi & Co. Ltd.
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Hayashi Kunio
Shionogi Research Laboratories Shionogi & Co. Ltd.
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