|
【结 构 式】 
|
【分子编号】65837 【品名】7-benzyloxy-4-chloro-5-(tetrahydropyran-4-yloxy)quinazole 【CA登记号】 |
【 分 子 式 】C20H19ClN2O3 【 分 子 量 】370.83524 【元素组成】C 64.78% H 5.16% Cl 9.56% N 7.55% O 12.94% |
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：(I)Condensation of 7-benzyloxy-4-chloro-5-(tetrahydropyran-4-yloxy)quinazole (I) with 5-chloro-1,3-benzodioxol-4-amine (II) by means of HCl in isopropanol gives the secondary amine (III), which is debenzylated by means of H2 over Pd/C in ethanol/THF to yield the 7-hydroxyquinazoline derivative (IV). Finally, this compound is condensed with 1-(2-hydroxyethyl)-4-methylpiperazine (V) by means of DBAD and PPh3 in dichloromethane (1). Scheme 1.
| 【1】 Ple, P., Hennequin, L.F.A. (AstraZeneca AB; AstraZeneca plc). Quinazoline derivatives for the treatment of tumours. CA 2407371, EP 1292594, JP 2003535859, US 2004214841, US 2006258642, US 7049438, WO 2001094341. |
| 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) | 65837 | 7-benzyloxy-4-chloro-5-(tetrahydropyran-4-yloxy)quinazole | C20H19ClN2O3 | 详情 | 详情 | |
| (II) | 65838 | 5-chloro-1,3-benzodioxol-4-amine; 5-Chlorobenzo[1,3]dioxol-4-ylamine | 379228-45-2 | C7H6ClNO2 | 详情 | 详情 |
| (III) | 65839 | C27H24ClN3O5 | 详情 | 详情 | ||
| (IV) | 65840 | C20H18ClN3O5 | 详情 | 详情 | ||
| (V) | 32589 | 2-(4-methyl-1-piperazinyl)-1-ethanol | 5464-12-0 | C7H16N2O | 详情 | 详情 |
Extended Information