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【结 构 式】 
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【药物名称】JANEX-3, WHI-P180 【化学名称】3-(6,7-Dimethoxyquinazolin-4-ylamino)phenol 【CA登记号】153437-55-9 【 分 子 式 】C16H15N3O3 【 分 子 量 】297.31625 |
【开发单位】AstraZeneca (Originator), Parker Hughes Institute (Originator) 【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, IMMUNOMODULATING AGENTS, RESPIRATORY DRUGS, Treatment of Transplant Rejection, EGFR (erbB1) Inhibitors, Jak3 Inhibitors, Mediator Release Inhibitors, TNF-alpha Release Inhibitors |
合成路线1
The cyclization of 4,5-dimethoxyanthranilic acid (I) with formamide by heating at 190 C gives 6,7-dimethoxyquinazoline (II), which is treated with refluxing SOCl2 to yield 4-chloro-6,7-dimethoxyquinazoline (III). Finally, this compound is condensed with 3-aminophenol (IV) in refluxing THF.
| 【1】 Barker, A.J. (AstraZeneca plc); Quinazoline derivs.. CA 2086968; EP 0566226; JP 1994073025; US 5616582 . |
| 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) | 23763 | 2-amino-4,5-dimethoxybenzoic acid | 5653-40-7 | C9H11NO4 | 详情 | 详情 |
| (II) | 23764 | 6,7-dimethoxyquinazoline; 6-methoxy-7-quinazolinyl methyl ether | C10H10N2O2 | 详情 | 详情 | |
| (III) | 23765 | 4-chloro-6,7-dimethoxyquinazoline; 4-chloro-6-methoxy-7-quinazolinyl methyl ether | C10H9ClN2O2 | 详情 | 详情 | |
| (IV) | 23766 | 3-aminophenol | 591-27-5 | C6H7NO | 详情 | 详情 |
Extended Information