A Short-Step Synthesis of Orally Active Carbapenem Antibiotic CS-834

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概要

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• An orally bioavailable carbapenem CS-834,which is a pivaloyloxymethyl (POM) ester-type prodrug and has (R)-5-oxopyrrolidin-3-ylthio moiety at the C-2 position of the 1β-methylcarbapenem skeleton, is currently under clinical trial. We accomplished a short-step synthesis of CS-834 by using phosphorus ylide from the intramolecular Wittig-type reaction in the key step for cyclization to the bicyclic carbapenem system. The POM ester group was found to be suitable for the cyclization conditions.

• 公益社団法人日本薬学会の論文
• 2000-01-01

著者

• Mori Makoto

  Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.

• OIDA Sadao

  Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd.

• Oida S

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• Oida Sadao

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

• Mori Makoto

  Medicinal Chemistry Research Laboratories Sankyo Co. Ltd.

関連論文

• Design, Synthesis and Antifungal Activity of the Novel Water-Soluble Prodrug of Antifungal Triazole CS-758
• Synthesis in Vitro Antifungal Activities of Novel Triazole Antifungal Agent CS-758
• Stereocontrolled Synthesis of Piperidine-Condensed Tricyclic Carbapenems (5-Azatrinems) and Their Antibacterial Activities
• Synthesis and Antifungal Activities of R-102557 and Related Dioxane-Triazole Derivatives
• A Short-Step Synthesis of Orally Active Carbapenem Antibiotic CS-834

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