4 years ago

Synthesis of Spirocyclic Pyrrolidines: Advanced Building Blocks for Drug Discovery

Synthesis of Spirocyclic Pyrrolidines: Advanced Building Blocks for Drug Discovery
Oksana O. Yanshyna, Pavel K. Mykhailiuk, Konstantin S. Gavrilenko, Tetiana V. Druzhenko, Maryna V. Butko, Bohdan A. Chalyk
The cover picture shows novel building blocks for drug discovery—spirocyclic pyrrolidine. The synthesis starts from common four-, five-, six- and seven-membered-ring ketones and includes only two chemical steps. The key transformation is the reaction between electron-deficient exocyclic alkenes and in situ generated N-benzyl azomethine ylide. The high potential of the developed method was demonstrated by the novel synthesis of the central core of the known antibacterial agents Sitafloxacin and Olamufloxacin. More information can be found in the Full Paper by P. K. Mykhailiuk et al. (DOI: 10.1002/chem.201704329).

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201704329

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