1620523-75-2Relevant academic research and scientific papers
An efficient synthesis of (3S,5S)-5-[3,3-dimethyl-1-(o-tolyl)-6-OXO-2H- pyridin-4-YL]- piperidine-3-carboxamide as potent renin inhibitor
Mori, Yutaka,Iwamoto, Mitsuhiro,Mori, Kazuki,Yoshida, Masao,Honda, Takeshi,Nagayama, Takahiro,Nishi, Takahide
, p. 1413 - 1426 (2014/07/07)
We report synthesis and biological evaluation of (3S,5S)-5-[3,3- dimethyl-1-(o-tolyl)-6-oxo-2H-pyridin-4-yl]piperidine-3-carboxamide as renin inhibitor. This effective synthetic route involves a zinc mediated Barbier reaction and an intramolecular Horner-Wadsworth-Emmons reaction of sterically hindered ketone as key reactions. The prepared compound 4 exhibited both potent renin inhibitory activity and significant in vivo efficacy in furosemide pretreated cynomolgus monkeys.
