Abbott-49816, A-49816
Chemical Name: Ethyl [2,3-dichloro-4-(3-aminomethyl-4-hydroxybenzoyl)phenoxy]acetate hydrochloride
CAS No. 78235-46-8, 78235-72-0 (free base)
项目整合开发状态: Clinical
项目研究机构: Abbott (Originator)
合成路线:Friedel-Crafts acylation of 2,3-dichlorophenetole with 4-methoxybenzoyl chloride gives the substituted benzophenone (I).Selective cleavage of the ethyl ether in (I) with AlCl3 produces phenol (II).Alkylation of (II) with ethyl bromoacetate is followed by heating with 48% HBr to give the phenoxyacetic acid derivative (III).Amidomethylation of (III) using the Tscherniac-Einhorn procedure gives (IV),which affords A-49816 after hydrolysis with HCl/EtOH.
📌 参考资料/链接：
参考文献标题:A-49816
文献作者:Luther,R.R.; Plattner,J.J.
参考来源:Drugs Fut 1988,13(12),1039
📄 详细内容
合成路线:Friedel-Crafts acylation of 2,3-dichlorophenetole with 4-methoxybenzoyl chloride gives the substituted benzophenone (I).Selective cleavage of the ethyl ether in (I) with AlCl3 produces phenol (II).Alkylation of (II) with ethyl bromoacetate is followed by heating with 48% HBr to give the phenoxyacetic acid derivative (III).Amidomethylation of (III) using the Tscherniac-Einhorn procedure gives (IV),which affords A-49816 after hydrolysis with HCl/EtOH.
参考文献标题:[(Aminomethyl)aryloxy]acetic acid esters.A new cl
文献作者:Lee,C.-M.; Plattner,J.J.; Ours,C.W.; Horrom,B.W.; Smital,J.R.; Pernet,A.G.; Bunnell,P.R.; El Masry,S.E.; Dodge,P.W.
参考来源:J Med Chem 1984,271579
产品链接: CAS No. 78235-46-8›› 产品链接: CAS No.78235-72-0››