Compound 1 (1-benzyl-3-methyl-4-[4-(4-fluorophenyl)-4-oxobutyl] piperazine), a synthetic intermediate identified as a potential atypical antipsychotic, was selected as the starting point for pharmacological improvement. From 1, sequential structural variations were conducted in order to improve its potency and oral bioavailability. These variations included a series of piperazine, ethanediamine, and piperidine derivatives. The piperidine series ...
[Armstrong, Alan; Pullin, Robert D. C.; Jenner, Chloe R.; Foo, Klement; White, Andrew J. P.; Scutt, James N. Tetrahedron Asymmetry, 2014 , vol. 25, # 1 p. 74 - 86]