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.