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【结 构 式】 
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【药物名称】Azelastine hydrochloride, W-2979M, E-0659, A-5610, Optivar, Azep, Corifina, Optilast, Afluon, Radethazin, Astelin, Allergodil, Rhinolast, Azeptin 【化学名称】4-(4-Chlorobenzyl)-2-(1-methylperhydroazepin-4-yl)phthalazin-1(2H)-one hydrochloride 【CA登记号】37932-96-0, 58581-89-8 (free base), 79307-93-0 (monoHCl) 【 分 子 式 】C22H25Cl2N3O 【 分 子 量 】418.37005 |
【开发单位】Asta Medica (Originator), Eisai (Licensee), MedPointe (Licensee), Bausch & Lomb (Comarketer), Sepracor (Comarketer) 【药理作用】Antiallergic Ophthalmic Agents, Drugs for Allergic Rhinitis, Ocular Antiinflammatory and Antiinfective Agents, OCULAR MEDICATIONS, Ophthalmic Drugs, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders, Histamine H1 Antagonists |
合成路线1
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.
| 【1】 Vogelsong, D.; et al.; Basically substituted benzyl phthalazone derivatives acid salts thereof and process for the production thereof. US 3813384 . |
| 【2】 Hillier, K.; Blancafort, P.; Castaner, J.; Serradell, M.N.; Azelastine. Drugs Fut 1980, 5, 3, 123. |