Studies on 3-Substituted 1,2-Benzisoxazole Derivatives. I
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概要
- 論文の詳細を見る
3-Amidinomethyl- (8), 3-imidazolinylmethyl- (9) and 3-tetrahydropyrimidinylmethyl-1,2-benzisoxazole (10) were synthesized from 1,2-benzisoxazole-3-acetonitrile (4) via iminoether (7). 3-Tetrazolylmethyl-1,2-benzisoxazole (5) and 1,2-benzisoxazole-3-acetamide oxime (11) were also prepared from 4. 3-Aminoethyl-1,2-benzisoxazole (25), a tryptamine analogue of 1,2-benzisoxazole, was synthesized from 3-chloroethyl-1,2-benzisoxazole (20). The bromination of 1,2-benzisoxazole-3-acetic acid (1) with one molar equivalent of bromine afforded α-bromo-1,2-benzisoxazole-3-acetic acid (27), which was decarboxylated to give 3-bromomethyl-1,2-benzisoxazole (30). The amination of 30 afforded 3-amino-methyl-1,2-benzisoxazole (31). The bromination of 1 with excess of bromine gave 3-tribromomethyl-1,2-benzisoxazole (28). N-Substituted 1,2-benzisoxazolylglycine ester (32) was synthesized from methyl α-bromo-1,2-benzisoxazole-3-acetate (29) which was obtained by the bromination of methyl 1,2-benzisoxazole-3-acetate (2).
- 公益社団法人日本薬学会の論文
- 1976-04-25
著者
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西村 温樹
Research Laboratories:dainippon Pharmaceutical Co. Ltd.
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西村 温樹
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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宇野 準
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
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宇野 準
大日本製薬株式会社総合研究所
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黒川 美貴雄
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
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長束 輝
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
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大和 穰
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.
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宇野 準
大日本製薬株式会社
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大和 穰
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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長束 輝
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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黒川 美貴雄
大日本製薬株式会社創薬研究所
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宇野 準
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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