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【结 构 式】 
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【药物名称】Cetirizine hydrochloride, P-071, Alerlisin, Virlix, Reactine, Zyrtec 【化学名称】(±)-[2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid dihydrochloride 【CA登记号】83881-51-0 (free base) 【 分 子 式 】C21H27Cl3N2O3 【 分 子 量 】461.81994 |
【开发单位】UCB (Originator), Daiichi Pharmaceutical (Licensee), Lacer (Licensee), Menarini (Licensee), Pfizer (Licensee), Sanofi-synthélabo (Licensee), Sumitomo Pharmaceuticals (Licensee) 【药理作用】Allergic Skin Disorders, Treatment for, Antiallergy/Antiasthmatic Drugs, Asthma Therapy, DERMATOLOGIC DRUGS, Drugs for Allergic Rhinitis, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders, Urticaria, Treatment for, Histamine H1 Antagonists |
合成路线1
The condensation of 1-(4-chlorodiphenylmethyl)piperazine (I) with methyl 2-(2-chloroethoxy)acetate (II) by means of Na2CO3 in refluxing xylene gives methyl 2-[2-[4-(4-chlorodiphenylmethyl)-1-piperazinyl]ethoxy]acetate (III), which is then hydrolyzed with KOH tn reftuxing ethanol.
| 【1】 Baltes, E.; De Lannoy, J.; Rodriguez, L. (UCB SA); Novel 2-[4-(diphenylmethyl)-1-piperazinyl]acetic acids and their amides, process for their preparation and pharmaceutical compsns. Containing them. EP 0058146; US 4525358 . |
| 【2】 Castaner, J.; Serradell, M.N.; Castaner, R.M.; Cetirizine Hydrochloride. Drugs Fut 1987, 12, 7, 624. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 28775 | p-Chloro benzhydryl piperazine; 1-[(4-Chlorophenyl)(phenyl)methyl]piperazine; N-(Chloro-1-benzhydryl)piperazine; 1-(4-Chlorobenzhydryl)piperazine | 303-26-4 | C17H19ClN2 | 详情 | 详情 |
| (II) | 16841 | methyl 2-(2-chloroethoxy)acetate | C5H9ClO3 | 详情 | 详情 | |
| (III) | 28776 | methyl 2-(2-[4-[(4-chlorophenyl)(phenyl)methyl]-1-piperazinyl]ethoxy)acetate | C22H27ClN2O3 | 详情 | 详情 |