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【结 构 式】 
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【药物名称】DV-182 【化学名称】8-[2-[4-(2,5-Dichlorophenyl)piperazin-1-yl]-1-methylethyl]-8-azaspiro[4.5]decane-7,9-dione 【CA登记号】 【 分 子 式 】C22H29Cl2N3O2 【 分 子 量 】438.40133 |
【开发单位】Recordati (Originator) 【药理作用】Atherosclerosis Therapy, CARDIOVASCULAR DRUGS, RENAL-UROLOGIC DRUGS, Treatment of Disorders of the Coronary Arteries and Atherosclerosis, Urinary Incontinence Therapy, alpha1D-Adrenoceptor Antagonists |
合成路线1
Mitsunobu coupling of 3,3-tetramethyleneglutarimide (I) with 1-chloro-2-propanol (II) afforded the N-(2-chloro-1-methylethyl) glutarimide (III). This was then condensed with N-(2,5-dichlorophenyl)piperazine (IV) in the presence of Et3N at 180 C to furnish the title compound.
| 【1】 Testa, R.; Leonardi, A.; Motta, G.; Barlocco, D. (Recordati Industria Chimica e Farmaceutica SpA); Cyclic amides and imides having selective antagonist activity at alpha-1D adrenergic receptor. WO 0105765 . |
| 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) | 28020 | 8-azaspiro[4.5]decane-7,9-dione | 1075-89-4 | C9H13NO2 | 详情 | 详情 |
| (II) | 33274 | 1-chloro-2-propanol; 1-chloroisopropanol | 127-00-4 | C3H7ClO | 详情 | 详情 |
| (III) | 45770 | 8-(2-chloro-1-methylethyl)-8-azaspiro[4.5]decane-7,9-dione | C12H18ClNO2 | 详情 | 详情 | |
| (IV) | 45771 | 1-(2,5-dichlorophenyl)piperazine | 1013-27-0 | C10H12Cl2N2 | 详情 | 详情 |
Extended Information