Novel benzothiophene H1-antihistamines for the treatment of insomnia was written by Moree, Wilna J.;Jovic, Florence;Coon, Timothy;Yu, Jinghua;Li, Bin-Feng;Tucci, Fabio C.;Marinkovic, Dragan;Gross, Raymond S.;Malany, Siobhan;Bradbury, Margaret J.;Hernandez, Lisa M.;O’Brien, Zhihong;Wen, Jianyun;Wang, Hua;Hoare, Samuel R. J.;Petroski, Robert E.;Sacaan, Aida;Madan, Ajay;Crowe, Paul D.;Beaton, Graham. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Synthetic Route of C6H3FN2 This article mentions the following:
SAR of lead benzothiophene H1-antihistamine I (R = 2-pyridyl) was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H1-antihistamines with a range of projected half-lives in humans were identified. Had a suitable human half-life as demonstrated in a human microdose study, but variability in pharmacokinetic profile, attributed to metabolic clearance, prevented further development of this compound I (R = 1-pyrazolyl) demonstrated lower predicted clearance in preclin. studies, and may represent a more suitable backup compound In the experiment, the researchers used many compounds, for example, 6-Fluoropicolinonitrile (cas: 3939-15-9Synthetic Route of C6H3FN2).
6-Fluoropicolinonitrile (cas: 3939-15-9) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Synthetic Route of C6H3FN2