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【结 构 式】 
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【分子编号】65714 【品名】N-(3-Chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine 【CA登记号】314771-88-5 |
【 分 子 式 】C18H14ClFN4O4 【 分 子 量 】404.7848232 【元素组成】C 53.41% H 3.49% Cl 8.76% F 4.69% N 13.84% O 15.81% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(IX)The aminoquinazoline precursor (I) is prepared by condensation of 4-(3-chloro-4-fluorophenylamino)-7-fluoro-6-nitroquinazoline (VII) with 3(R)-hydroxytetrahydrofuran (VIII) by means of potassium tert-butoxide in DMF to yield the tetrahydrofuranyloxyquinazoline (IX), which is then reduced at the nitro group by catalytic hydrogenation over PtO2 (1). Scheme 2.
| 【1】 Himmelsbach, F., Langkopf, E., Solca, F., Jung, B., Baum, A., Blech, S. (Boehringer Ingelheim Pharma GmbH & Co., KG). Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof. DE 10063435, EP 1345910, JP 2004516283, US 2002173509, US 2006100223, US 7019012, WO 0250043. |
| 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) | 65710 | N4-(3-Chloro-4-fluorophenyl)-7-[[(3S)-tetrahydro-3-furanyl]oxy]-4,6-quinazolinediamine | 314771-76-1 | C18H16ClFN4O2 | 详情 | 详情 |
| (VII) | 54956 | N-(3-chloro-4-fluorophenyl)-7-fluoro-6-nitro-4-quinazolinamine; N-(3-chloro-4-fluorophenyl)-N-(7-fluoro-6-nitro-4-quinazolinyl)amine | 162012-67-1 | C14H7ClF2N4O2 | 详情 | 详情 |
| (VIII) | 44420 | (3S)-tetrahydro-3-furanol; (S)-3-Hydroxytetrahydrofuran | 86087-23-2 | C4H8O2 | 详情 | 详情 |
| (IX) | 65714 | N-(3-Chloro-4-fluorophenyl)-6-nitro-7-[[(3S)-tetrahydro-3-furanyl]oxy]-4-quinazolinamine | 314771-88-5 | C18H14ClFN4O4 | 详情 | 详情 |
Extended Information