Synthetic Studies on Diuretics. 5-(3,3-N, S-Substituted-2-propenoyl)-2,3-dihydro-2-benzo[b]furancarboxylic Acids
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概要
- 論文の詳細を見る
6,7-Dichloro-2,3-dihydro-2-benzo[b]furancarboxylic acid derivatives having a 3,3-N, S-disubstituted-2-propenoyl group at the 5-position were prepared by alkylation of 5-(thiocarbamoyl)acetyl derivatives of the 2,3-dihydro-2-benzo[b]furancarboxylic acid ester or by acetal exchange reaction of 5-[3,3-bis(alkylthio)-2-propenoyl] derivatives. Synthesis of 5-[4 and/or 5-(di)substituted-4-thiazolin-2-ylidene]acetyl-2,3-dihydro-2-benzo[b]furancarboxylic acids was also achieved by the reaction of 2-halo-1-methoxyethyl isothiocyanate with the 5-acetyl derivative in the presence of base or through sulfide contraction of 2-[((6,7-dichloro-2-methoxycarbonyl-2,3-dihydrobenzo[b]furan-5-yl)carbonyl)methylthio]thiazolium bromide. Some of the compounds which were synthesized showed potent natriuretic activities in rats and mice. The structure-activity relationship is also discussed.
- 公益社団法人日本薬学会の論文
- 1989-05-25
著者
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中村 益久
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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中村 益久
Shionogi Research Laboratories Shionogi & Co. Ltd.
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大杉 栄一
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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藤岡 紀洋
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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原田 紘
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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前田 量三
Shionogi Research Laboratories, Shionogi & Co., Ltd.,
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藤岡 紀洋
Shionogi Research Laboratories Shionogi & Co. Ltd.
-
原田 紘
Shionogi Research Laboratories Shionogi & Co. Ltd.
-
前田 量三
Shionogi Research Laboratories Shionogi & Co. Ltd.
-
大杉 栄一
Shionogi Research Laboratories Shionogi & Co. Ltd.
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