Racemization Kinetics of Meluadrine Tartrate in Aqueous Solution
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概要
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The kinetics of racemization of meluadrine tartrate in aqueous solution was investigated by HPLC, over the pH range of 1.2 to 12 at 40, 60 and 80℃. The racemization was followed by measuring both the residual(R)-enantiomer and formed(S)-enantiomer of meluadrine. The pH-racemization rate profile of meluadrine showed a minimum racemization rate constant between pH 4 and 6, and the rate constant increased rapidly with decreasing pH below pH 3. In the basic region, the racemization rate constant showed a maximum at around pH 9. Four pathways of racemization of meluadrine are proposed, depending on the dissociation state of the phenolic and amino groups. The calculated racemization rate-pH profile agreed well with the observations. The values of activation energy(95-115kJ/mol)suggest that a similar quinoid intermediate is involved throughout the pH range examined. The objective of this study is to clarify the racemization mechanism of benzylalcohol derivative with phenoric group. This study offers fundamental knowledge for the other benzylalcohol derivatives, which have similar moiety structure.
- 公益社団法人日本薬学会の論文
- 2001-01-01
著者
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Tsuji Akira
金沢大学 薬
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Tsuji Akira
富山化学工業綜合研究所
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山城 祐子
Faculty Of Pharmaceutical Sciences Kobe Gakuin University
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山本 譲
Faculty Of Pharmaceutical Sciences Kanazawa University
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Tsuji A
Kanazawa Univ. Ishikawa Jpn
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Matsuo Keizo
近畿大学 薬
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Nagata O
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Tsuji Akira
Department Of Pediatrics:hospital Pharmacy:and Faculty Of Pharmaceutical Sciences University Of Kana
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Nagata Osamu
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Yamamoto Y
Tohoku Univ. Sendai Jpn
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Kato H
Research And Development Headquarters Hokurikit Seiyaku Co. Ltd.
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Yamamoto Y
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Kado Noriyuki
Research And Development Division Hokuriku Seiyaku Co. Ltd.
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Yamamoto Y
School Of Pharmaceutical Sciences Toho University
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MATSUO Kazuya
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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YAMAMOTO Youichi
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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KADO Noriyuki
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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YAMAZAKI Masahiro
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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NAGATA Osamu
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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KATO Hideo
Pharmaceutical Research Laboratory, Hokuriku Seiyaku Co., Ltd.
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Yamamoto Youichi
Pharmaceutical Research Laboratory Hokuriku 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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Matsuo Kazuya
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.:department Of Pharmaceutics Kanazawa Un
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Yamamoto Yoshio
Pharmaceutical Research Division Takeda Chemical Industries Ltd.
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Kato Hideo
Nihon Bioresearch Inc.
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Tsuji Akira
Department Of Molecular Pharmaceutics Graduate School Of Natural Science And Technology Kanazawa Uni
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Yamazaki Masahiro
Pharmaceutical Research Laboratory Hokuriku Seiyaku Co. Ltd.
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Yamamoto Y
大阪薬科大学
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Nagata O
Narch
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Kato Hideo
Yamaguchi Univ. Yamaguchi Jpn
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山本 靖夫
School Of Pharmaceutical Sciences Toho University
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