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项目整合精选>>>Azelastine hydrochloride, W-2979M, E-0659, A-5610, Optivar, Azep, Corifina, Optilast, Afluon, Radethazin, Astelin, Allergodil, Rhinolast, Azeptin
Azelastine hydrochloride, W-2979M, E-0659, A-5610, Optivar, Azep, Corifina, Optilast, Afluon, Radethazin, Astelin, Allergodil, Rhinolast, Azeptin
1(2H)-邻苯他嗪酮,4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-阿氮平-4-基)-盐酸盐(1:) 盐酸氮卓斯汀 盐酸氮卓斯汀Chemical Name: 4-(4-Chlorobenzyl)-2-(1-methylperhydroazepin-4-yl)phthalazin-1(2H)-one hydrochloride
CAS No. 37932-96-0, 58581-89-8 (free base), 79307-93-0 (monoHCl)
项目整合开发状态: Launched-1986
项目研究机构: Asta Medica (Originator), Eisai (Licensee), MedPointe (Licensee), Bausch & Lomb (Comarketer), Sepracor (Comarketer)
合成路线:The cyclization of alpha-(p-chlorophenyl)acetophenone-o-carboxylic acid (I) with hydrazine sulfate by means of NaOH in water gives 4-(p-chlorobenzyl)-1-(2H)-phthalazinone (II),which is then condensed with 2-(2-chloroethyl)-N-methylpyrrolidine (III) by means of NaOH in hot water.
📌 参考资料/链接：
参考文献标题:Azelastine
文献作者:Hillier,K.; Blancafort,P.; Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1980,5(3),123
📄 详细内容
合成路线:The cyclization of alpha-(p-chlorophenyl)acetophenone-o-carboxylic acid (I) with hydrazine sulfate by means of NaOH in water gives 4-(p-chlorobenzyl)-1-(2H)-phthalazinone (II),which is then condensed with 2-(2-chloroethyl)-N-methylpyrrolidine (III) by means of NaOH in hot water.
参考文献标题:Basically substituted benzyl phthalazone derivatives acid salts thereof and process for the production thereof
文献作者:Vogelsong,D.; et al.
参考来源:US 3813384