Synthesis of the Metabolites of 4-(2-Methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide (KRP-197/ONO-8025)
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概要
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We synthesized the six presumed metabolites (2-7) of 4-(2-methyl-1h-imidazol-1-yl)-2,2-diphenylbutanamide [KRP-197/ONO-8025, 1], a urinary incontinence therapeutic agent, in order to confirm the structures of the metabolites. Metabolite (2) was synthesized via glucuronidaion of compound (1) and methyl 2,3,4-tri-O-benzoyl-1-methanesulfonyl-α-D-glucopyranuronate. Metabolite (3) was synthesized via 3-(tert-butoxycarbonyl)-2-methyl-1,3-imidazolidine-4,5-dione. Metabolites (4-7) were synthesized via 4-amino-2-diphenylbutanamide, respectively. The structures of the metabolites (2-7) in humans were identified by means of synthesis of the authentic compounds.
- 社団法人日本薬学会の論文
- 2007-07-01
著者
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AKITA Hiroyuki
School of Pharmaceutical Science, Toho University
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Numata Makoto
Research Center Kyorin Pharmaceutical Co. Ltd.
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ARAYA Ichiro
Research Center, Kyorin Pharmaceutical Co., Ltd.
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TSUBUKI Takeshi
Research Center, Kyorin Pharmaceutical Co., Ltd.
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SAITO Tatsuhiro
Research Center, Kyorin Pharmaceutical Co., Ltd.
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Araya Ichiro
Res. Center Kyorin Pharmaceutical Co. Ltd.
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Araya Ichiro
Research Center Kyorin Pharmaceutical Co. Ltd.:faculty Of Pharmaceutical Sciences Toho University
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Akita Hiroyuki
School Of Parmaceutical Sciences Toho University
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Saito Tatsuhiro
Research Center Kyorin Pharmaceutical Co. Ltd.
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Tsubuki Takeshi
Research Center Kyorin Pharmaceutical Co. Ltd.
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