Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 23, Issue 66, Pages 16782-16786Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201702362
Keywords
azomethine ylides; building blocks; drug discovery; pyrrolidines; spirocycles
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In the context of drug discovery, novel spirocyclic pyrrolidines have been synthesized in two steps from common three- to seven-membered-ring (hetero)alicyclic ketones. The key transformation is a reaction between an electron-deficient exocyclic alkene and an in situ generated N-benzyl azomethine ylide. The developed method has been used to synthesize the central diamine core of the known antibacterial agents Sitafloxacin and Olamufloxacin.
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