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【结 构 式】 
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【药物名称】EC-665, SDZ-249-665 【化学名称】N-[4-(2-Aminoethoxy)-3-methoxybenzyl]-N'-(4-tert-butylbenzyl)urea hydrochloride 【CA登记号】189215-75-6 【 分 子 式 】C22H32ClN3O3 【 分 子 量 】421.97164 |
【开发单位】Novartis (Originator) 【药理作用】ANALGESIC AND ANESTHETIC DRUGS, Analgesic Drugs, Neuropathic Pain, Treatment of, Non-Opioid Analgesics |
合成路线1
Isocyanate (II) was prepared by treatment of 4-tert-butylbenzylamine (I) with phosgene in refluxing toluene. Subsequent coupling of isocyanate (II) with 4-(2-phthalimidoethoxy)-3-methoxybenzylamine (III) furnished urea (IV). The phthaloyl protecting group was then removed by hydrazinolysis. The resulting amine was finally converted to the corresponding hydrochloride salt.
| 【1】 Campbell, E.A.; Walpole, C.S.J. (Novartis AG; Novartis Deutschland GmbH); Urea derivs. and their use as analgesics and antiinflammatory agents. WO 9711052 . |
| 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) | 47899 | 4-(tert-butyl)benzylamine; [4-(tert-butyl)phenyl]methanamine | 39895-55-1 | C11H17N | 详情 | 详情 |
| (II) | 47900 | 1-(tert-butyl)-4-(isocyanatomethyl)benzene; 4-(tert-butyl)benzyl isocyanate | C12H15NO | 详情 | 详情 | |
| (III) | 47901 | 2-[2-[4-(aminomethyl)-2-methoxyphenoxy]ethyl]-1H-isoindole-1,3(2H)-dione | C18H18N2O4 | 详情 | 详情 | |
| (IV) | 47902 | N-[4-(tert-butyl)benzyl]-N'-[4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]-3-methoxybenzyl]urea | C30H33N3O5 | 详情 | 详情 |
Extended Information