A Short-Step Synthesis of Orally Active Carbapenem Antibiotic CS-834.
Chemical & pharmaceutical bulletin/Chemical and pharmaceutical bulletin(2000)
摘要
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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关键词
carbapenem,synthesis,intramolecular Wittig-type reaction,pivaloyloxymethyl ester,diethyl ethylphosphonite,prodrug
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