An Improved Synthesis of Butyl 4-[(4-Amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (AU-224)
スポンサーリンク
概要
- 論文の詳細を見る
A new and facile route for the synthesis of the novel gastrointestinal prokinetic butyl 4-[(4-amino-5-chloro-2-methoxybenzoyl)amino]-1-piperidineacetate (1b), which exhibited potent gastro- and colon-prokinetic activities by oral administration without significant side effects, was established. The key intermediate, butyl 4-amino-1-piperidineacetate (16), was prepared from commercially available 4-amino-benzylpiperidine (2) in a high yield with four steps. Compound 1b was prepared by condensation of commercially available 4-amino-5-choloro-2-methoxybenzoic acid (7) with 16 in 84% yield. This improved synthetic route was appropriate for large-scale synthesis of 1b.
- 公益社団法人日本薬学会の論文
- 2001-06-01
著者
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斎藤 徹
Faculty Of Pharmaceutical Sciences Kanazawa University
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花岡 美代次
金沢大学薬学部
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HANAOKA Miyoji
Faculty of Pharmaceutical Sciences, Kanazawa University
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Nagata O
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Suzuki T
Drug Discovery Research Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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Sakaguchi J
Research Division Hokuriku Seiyaku Co. Ltd.
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Hanaoka Miyoji
Faculty Of Pharmaceutical Sciences Kanazawa University
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Nagata Osamu
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kato H
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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鈴木 徳治
千葉大 薬
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Suzuki T
Laboratory Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Chiba University
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KATO Hideo
Research and Development Division, Hokuriku Seiyaku Co., Ltd.,
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SUZUKI Tomio
Research and development Division, Hokuriku Seiyaku Co., Ltd.,
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SAKAGUCHI Jun
Research Division, Hokuriku Seiyaku Co., Ltd.
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HIGASHI Taijiro
Research Division, Hokuriku Seiyaku Co., Ltd.
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AZUMA Takahiro
Research Division, Hokuriku Seiyaku Co., Ltd.
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IWASAKI Nobuhiko
Research Division, Hokuriku Seiyaku Co., Ltd.
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KONDO Noriyuki
Research Division, Hokuriku Seiyaku Co., Ltd.
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Kado Noriyuki
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Higashi Taijiro
Research Division Hokuriku Seiyaku Co. Ltd.
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Saito T
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Saito Takako
Research And Development Laboratories Maruho Co. Ltd.
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KADO Noriyuki
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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Suzuki Toshikazu
Discovery Research Laboratory Tanabe Seiyaku Co. Ltd.
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Kado Noriyuki
Research And Development Headquaters Hokuriku Seivaku Co. Ltd.
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Kado Noriyuki
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Kato Hideo
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Kato Hideo
Nihon Bioresearch Inc.
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Nagata O
Narch
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Iwasaki N
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Suzuki T
Research Unit Of Pharmaceutics College Of Pharmacy Nihon University
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Sugihara T
Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Saito T
Research And Development Laboratories Maruho Co. Ltd.
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Azuma Takahiro
Research Division Hokuriku Seiyaku Co. Ltd.
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Hattori Masao
Metabolic Engineering Institute Of Natural Medicine University Of Toyama
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Kato Hideo
Yamaguchi Univ. Yamaguchi Jpn
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花岡 美代次
Institute Of Natural Medicine University Of Toyama
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Iwasaki Nobuhiko
Research and Development Division, Hokuriku Seiyaku Co., Ltd.
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