Synthesis of 5-(Substituted Alkyl) picolinic Acids. The Dopamine β-Hydroxylase Inhibitors. II
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概要
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The improved synthesis of 5-(4-chlorobutyl) picolinic acid (II), the potent dopamine β-hydroxylase inhibitor, was reported. The key intermediate, 2-cyclopropyl-5-cyclopropylcarbonylpyridine (IV) was converted to 5-(4-chlorobutyl)-2-cyclopropylpyridine (VII), which was directly oxidized with nitric acid to give II. Similarly, fusaric acid (I) was synthesized from 2-cyclopropyl-5-(cyclopropylhydroxy) methylpyridine (V).
- 公益社団法人日本薬学会の論文
- 1978-08-25
著者
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逆井 武次
Pharmaceutical Institute, Tohoku University
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濱野 弘明
Research Laboratory, Pharmaceutical Division, Nippon Kayaku Co., Ltd.
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濱野 弘明
Research Laboratory Pharmaceutical Division Nippon Kayaku Co. Ltd.
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宮野 耕一
Research Laboratory, Pharmaceutical Division, Nippon Kayaku Co., Ltd.
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逆井 武次
Research Laboratory, Pharmaceutical Division, Nippon Kayaku Co., Ltd.
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逆井 武次
Pharmaceutical Institute Tohoku University
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宮野 耕一
Research Laboratory Pharmaceutical Division Nippon Kayaku Co. Ltd.
関連論文
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- Studies on Dimethoxyphenylaminoalcohols. II. Syntheses and Relative Configulations of 1-Dimethoxyphenyl-3-(alkylamino) butanols
- Studies on Pyrimidine Derivatives. XV. Homolytic Acylation and Amidation of Simply Substituted Pyrimidines
- Synthesis of 5-(Substituted Alkyl) picolinic Acids. The Dopamine β-Hydroxylase Inhibitors. II
- Synthesis of 5-(Substituted Alkyl) Picolinic Acids, the Dopamine β-Hydroxylase Inhibitors. I
- Studies on Pyrimidine Derivatives. XXII. Site-selective Oxidation of Dimethylpyrimidines with Selenium Dioxide to Pyrimidine-minoaldehydes
- Studies on Pyrimidine Derivatives. XVI. Site Selectivity in the Homolytic Substitution of Simple Pyrimidines