Flupirtine maleate, D-9998, Katadolon
马来酸氟吡汀 氟吡汀 Chemical Name: 2-Amino-3-carbethoxyamino-6-(p-fluorobenzylamino)pyridine maleate
CAS No. 75507-68-5, 56995-20-1 (free base)
项目整合开发状态: Launched-1986
项目研究机构: Asta Medica (Originator), AWD.pharma (Licensee), Lindopharm (Licensee)
合成路线:The reaction of 2,6-dichloro-3-nitropyridine (I) with ammonia yields 2-amino-3-nitro-chloropyridine (II).4-Fluorobenzylamine (III) reacts in dioxane and in the presence of triethylamine with (II),resulting in the 2-amino-3-nitro-6-p-fluorobenzylamine derivative (IV).The latter is hydrated and in situ the 3-amino group is condensed with ethyl chloroformate leading to the stable 2-amino-3-carbethoxyamino-6-(p-fluorobenzylamino)pyridine (Flupirtine).
📌 参考资料/链接：
参考文献标题:Flupirtine
文献作者:Castar,J.; Serradell,M.N.; Blancafort,P.
参考来源:Drugs Fut 1983,8(9),773
📄 详细内容
合成路线:The reaction of 2,6-dichloro-3-nitropyridine (I) with ammonia yields 2-amino-3-nitro-chloropyridine (II).4-Fluorobenzylamine (III) reacts in dioxane and in the presence of triethylamine with (II),resulting in the 2-amino-3-nitro-6-p-fluorobenzylamine derivative (IV).The latter is hydrated and in situ the 3-amino group is condensed with ethyl chloroformate leading to the stable 2-amino-3-carbethoxyamino-6-(p-fluorobenzylamino)pyridine (Flupirtine).
参考文献标题:
文献作者:Thiele,K.; Steinmetz,G.; Bebenburg,W.v.
参考来源:Chem Ztg 1979,103(10),387
合成路线:The reaction of 2,6-dichloro-3-nitropyridine (I) with ammonia yields 2-amino-3-nitro-chloropyridine (II).4-Fluorobenzylamine (III) reacts in dioxane and in the presence of triethylamine with (II),resulting in the 2-amino-3-nitro-6-p-fluorobenzylamine derivative (IV).The latter is hydrated and in situ the 3-amino group is condensed with ethyl chloroformate leading to the stable 2-amino-3-carbethoxyamino-6-(p-fluorobenzylamino)pyridine (Flupirtine).
参考文献标题:
文献作者:Bebenburg,W.v.; Engel,J.; Sheldrick,W.S.; Thiele,K.
参考来源:Chem Ztg 1981,105(10),217
产品链接: CAS No. 75507-68-5›› 产品链接: CAS No.56995-20-1››