Arbidol, Arbidol
盐酸阿比朵尔Chemical Name: 6-Bromo-4-(dimethylaminomethyl)-5-hydroxy-1-methyl-2-(phenylthiomethyl)-1H-indole-3-carboxylic acid ethyl ester hydrochloride monohydrate
CAS No. 131707-23-8
项目整合开发状态: Launched-1992
项目研究机构: All-Russian Chem.-Pharm. Res. Inst. (Originator), Center for Chemistry of Drugs (Originator), Nauchno-Issledovatelsky Institut (Originator), Pfizer (Licensee)
合成路线:1,2-Dimethyl-5-hydroxyindole-3-acetic acid ethyl ester (I) is acetylated with acetic anhydride affording the O-acyl derivative (II),which is brominated to the corresponding dibromide compound (III).The reaction of (III) with thiophenol in KOH yields (IV),which is then submitted to a conventional Mannich condensation with formaldehyde and dimethylamine in acetic acid,giving the free base of arbidol (V),which is treated with aqueous hydrochloric acid.
📌 参考资料/链接：
参考文献标题:Ethyl ester 6-bromine-5-hydroxy-4-dimethyl-aminomethyl-1-methyl-2-phenylthiomethyl indole-3-carboxylic acid HCl H20,method of obtaining it and a pharmaceutical preparation of antiviral,interferon-inducing and immunomodulating action based on it
文献作者:Grinev,A.N.; Pershin,G.N.(All-Russian Chemical-Pharmaceutical Research Institute; Nauchno-Issledovatelsky Institut)
参考来源:US 5198552; WO 9008135
📄 详细内容
合成路线:1,2-Dimethyl-5-hydroxyindole-3-acetic acid ethyl ester (I) is acetylated with acetic anhydride affording the O-acyl derivative (II),which is brominated to the corresponding dibromide compound (III).The reaction of (III) with thiophenol in KOH yields (IV),which is then submitted to a conventional Mannich condensation with formaldehyde and dimethylamine in acetic acid,giving the free base of arbidol (V),which is treated with aqueous hydrochloric acid.
参考文献标题:Arbidol
文献作者:Glushkov,R.G.
参考来源:Drugs Fut 1992,17(12),1079
产品链接: CAS No. 131707-23-8››