l-084 has been researched along with azetidine* in 1 studies
1 other study(ies) available for l-084 and azetidine
Article | Year |
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A practical and facile synthesis of azetidine derivatives for oral carbapenem, L-084.
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 1beta-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. Topics: Administration, Oral; Azetidines; Carbapenems; Drug Industry; Humans; Molecular Structure; Stereoisomerism; Thiazoles | 2006 |