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Practical Synthesis of Fluorinated Piperidine Analogues Based on the 2-Azaspiro[3.3]heptane Scaffold

Synlett 2016, 27 (12), 1824-1827

DOI: 10.1055/s-0035-1562113

Chernykh A. V.; Tkachenko A. N.; Feskov I. O.; Daniliuc C. G.; Tolmachova N. A.; Volochnyuk D. M.; Radchenko D. S.

The synthesis of a set of conformationally restricted fluorinated analogues of piperidine, based on a 2-azaspiro[3.3]heptane scaffold, is reported. Different pattern of fluorine substitution within the rigid skeleton make the analogues excellent candidates for use in drug design. The overall simplicity of the experimental procedures and the availability of inexpensive starting materials allow for multigram-scale syntheses of the described compounds.

Practical Synthesis of Fluorinated Piperidine Analogues Based on the 2-Azaspiro[3.3]heptane Scaffold

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