A Practical and Facile Synthesis of Azetidine Derivatives for Oral Carbapenem, L-084
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概要
- 論文の詳細を見る
An orally active carbapenem L-084, which exhibits high bioavailability in humans, has a 1-(1,3-thiazolin-2-yl)azetidin-3-ylthio moiety at the C-2 position of the 1β-methylcarbapenem skeleton. We established a practical and cost-effective synthesis of 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine (1) for further scale-up production of L-084. This synthesis method entails an industry-oriented reaction of azetidine ring-closure to yield N-benzyl-3-hydroxyazetidine (16), which is eventually converted to 1 via key intermediates, Bunte salts 19 and 20.
- 公益社団法人日本薬学会の論文
- 2006-10-01
著者
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Nagao Yoshimitsu
Graduate School of Pharmaceutical Sciences, The University of Tokushima
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KUMAGAI Toshio
Medical Research Laboratories, Wyeth Lederle Japan, Ltd.
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長尾 善光
Graduate School Of Pharmaceutical Sciences The University Of Tokushima
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長尾 善光
徳島大学薬学部
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Nagao Yoshimitsu
Graduate School Of Pharmaceutical Sciences The University Of Tokushima
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Nagao Y
Faculty Of Pharmaceutical Sciences The University Of Tokushima
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Nagao Yoshimitsu
Faculity Of Pharmaceutical Sciences The University Of Tokushima
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Tamai Satoshi
Medical Research Laboratories Wyeth K.k.
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Kumagai Toshio
Medical Research Laboratories Wyeth K.k.
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Isoda Takeshi
Medical Research Laboratories Wyeth K.k.
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YAMAMURA Itsuki
Medical Research Laboratories, Wyeth K.K.
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Yamamura Itsuki
Medical Research Laboratories Wyeth K.k.
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Tamai Satoshi
Medical Research Laboratories
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Kumagai Toshio
Medical Research Laboratories
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Yamamura Itsuki
Medical Research Laboratories
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Isoda Takeshi
Medical Research Laboratories
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