新产品编号:509913

Chemical Name: 4-(Aminomethyl)-2,6-difluorophenol
CAS No. 220353-10-6 (hydrochloride)
项目整合开发状态: Biological Testing
项目研究机构: AstraZeneca (Originator)
合成路线:Nitration of 2,6-difluorophenol (I) gave 2,6-difluoro-4-nitrophenol (II),which was reduced to the corresponding aniline (III) by hydrogenation over Pd/C.Nitrile (IV) was obtained by diazotization of (III) followed by in situ displacement of the diazonium salt with CuCN and KCN.The nitrile (IV) was finally reduced to the title benzylamine employing borane in THF.
📌 参考资料/链接:
参考文献标题:2,6-Difluorophenol as a bioisostere of a carboxylic acid: Bioisosteric analogues of gamma-aminobutyric acid
文献作者:Qiu,J.; Stevenson,S.H.; O'Beirne,M.J.; Silverman,R.B.
参考来源:J Med Chem 1999,42(2),329