A practical and facile synthesis of azetidine derivatives for oral carbapenem, L-084

…, I Yamamura, S Tamai, T Kumagai, Y Nagao

文献索引：Isoda, Takeshi; Yamamura, Itsuki; Tamai, Satoshi; Kumagai, Toshio; Nagao, Yoshimitsu Chemical and Pharmaceutical Bulletin, 2006 , vol. 54, # 10 p. 1408 - 1411

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被引用次数: 18

摘要

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- ...