RX-72601
Chemical Name: cis-1-[2-(3-Hydroxyphenyl)cyclohexyl]-1-methylpyrrolidinium bromide
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:A mixture of 2-(3-methoxyphenyl)cyclohexanone (I),pyrrolidine (II) and formic acid is heated at 130-40 C to give cis-2-(3-methoxyphenyl)-1-pyrrolidylcyclohexane (III),which is demethylated with refluxing HBr (47%) giving cis-2-(3-hydroxyphenyl)-1-pyrrolidylcyclohexane (IV).Finally this tertiary amine is quaternized with CH3Br.
📌 参考资料/链接：
参考文献标题:RX 72601
文献作者:Casta馿r,J.; Hopkins,S.J.
参考来源:Drugs Fut 1976,1(6),304
📄 详细内容
合成路线:A mixture of 2-(3-methoxyphenyl)cyclohexanone (I),pyrrolidine (II) and formic acid is heated at 130-40 C to give cis-2-(3-methoxyphenyl)-1-pyrrolidylcyclohexane (III),which is demethylated with refluxing HBr (47%) giving cis-2-(3-hydroxyphenyl)-1-pyrrolidylcyclohexane (IV).Finally this tertiary amine is quaternized with CH3Br.
参考文献标题:Synthesis and biological evaluation of 2,3-diarylpyrazines and quinoxalines as selective COX-2 inhibitors
文献作者:Singh,S.K.; Saibaba,V.; Ravikumar,V.; Rudrawar,S.V.; Daga,P.; Rao,C.S.; Akhila,V.; Hedge,P.; Rao,Y.K.
参考来源:J Pharm Pharmac 1974,26(8),134
合成路线:A mixture of 2-(3-methoxyphenyl)cyclohexanone (I),pyrrolidine (II) and formic acid is heated at 130-40 C to give cis-2-(3-methoxyphenyl)-1-pyrrolidylcyclohexane (III),which is demethylated with refluxing HBr (47%) giving cis-2-(3-hydroxyphenyl)-1-pyrrolidylcyclohexane (IV).Finally this tertiary amine is quaternized with CH3Br.
参考文献标题:
文献作者:Lewis,J.W.(Reckitt & Colman Pharmaceuticals)
参考来源:FR 2187296