A short-step synthesis of orally active carbapenem antibiotic CS-834 |
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Authors: | Mori M Oida S |
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Affiliation: | Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan. |
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Abstract: | 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 1 beta-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. |
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