A-278637
Chemical Name: (-)-9(S)-(3-Bromo-4-fluorophenyl)-2,3,4,5,6,7,8,9-octahydrothieno[3,2- b]quinoline-8-one 1,1-dioxide
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The Hantzsch reaction between 3-oxotetrahydrothiophene-1,1-dioxide (I),3-bromo-4-fluorobenzaldehyde (II) and 3-amino-2-cyclohexen-1-one (III) in refluxing EtOH yielded the hydroxy tetrahydropyridine derivative (IV).Dehydration of the cyclic hemiaminal function of (IV) was carried out in refluxing toluene to produce the racemic dihydropyridine,which was resolved into the individual enantiomers by chiral HPLC.
📌 参考资料/链接：
参考文献标题:Potassium channel openers
文献作者:Drizin,I.; Holladay,M.W.; Carroll,W.A.; Zhang,H.Q.; Sullivan,J.P.(Abbott Laboratories Inc.)
参考来源:EP 1040097; US 6265417; WO 9931059
📄 详细内容
合成路线:The Hantzsch reaction between 3-oxotetrahydrothiophene-1,1-dioxide (I),3-bromo-4-fluorobenzaldehyde (II) and 3-amino-2-cyclohexen-1-one (III) in refluxing EtOH yielded the hydroxy tetrahydropyridine derivative (IV).Dehydration of the cyclic hemiaminal function of (IV) was carried out in refluxing toluene to produce the racemic dihydropyridine,which was resolved into the individual enantiomers by chiral HPLC.
参考文献标题:Novel sulfonyldihydropyridine potassium channel openers with potential utility in the treatment of overactive bladder (OAB)
文献作者:Drizin,I.; et al.
参考来源:222nd ACS Natl Meet (Aug 26 2001,Chicago) 2001,Abst MEDI 197