Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
(E)-3-(Benzenesulfonyl)-2-(methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine (7) was found to be a potent and selective 5-HT(6) antagonist. A one-step synthesis of this compound is described.
Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA. yong-jin.wu@bms.com
Yong-Jin
YJ
Wu
Huan
H
He
Shuanghua
S
Hu
Yazhong
Y
Huang
Paul M
PM
Scola
Katharine
K
Grant-Young
Robert L
RL
Bertekap
Dedong
D
Wu
Qi
Q
Gao
Yi
Y
Li
Cheryl
C
Klakouski
Ryan S
RS
Westphal
D000181:Acrylonitrile / Q000031:analogs & derivatives / Q000737:chemistry*; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D018360:Crystallography, X-Ray; D065607:Cytochrome P-450 Enzyme Inhibitors; D006801:Humans; D008958:Models, Molecular; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology
C479679:2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile; C479678:3-(benzenesulfonyl)-2-(methylsulfanyl)pyrido(1,2-a)pyrimidin-4-ylidenamine; D065607:Cytochrome P-450 Enzyme Inhibitors; D011743:Pyrimidines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013450:Sulfones; C097216:serotonin 6 receptor; D000181:Acrylonitrile; D002118:Calcium