|
【结 构 式】 
|
【分子编号】67677 【品名】1-(((6-methoxy-4-((5-(methylcarbamoyl)naphthalen-2-yl)oxy)quinolin-7-yl)oxy)methyl)cyclopropanecarbonyl azide 【CA登记号】 |
【 分 子 式 】C27H23N5O5 【 分 子 量 】497.51 【元素组成】C 65.18% H 4.66% N 14.08% O 16.08% |
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：(XLVI)Mitsunobu reaction of 4-chloro-6-methoxyquinolin-7-ol (XXXIII) with alcohol (XXXVI) using DEAD and PPh3 in THF yields adduct (XLV), which by Ullmann reaction with 6-hydroxy-N-methyl-1-naphthamide (V) in the presence of DMAP in 2,6-lutidine or i-PrOH at 130 °C or by means of Cs2CO3, CuI and picolinic acid or acetylacetone in DMF at 120 °C gives diaryl ether (XXXIX). This compound is alternatively obtained by Curtius rearrangement of azide (XLVI) with Pmb-OH in refluxing toluene .
| 【1】 Chen, G.P. (Advenchen Laboratories, LLC). Process for preparing the antitumor agent 6-(7-((1-aminocyclopropyl) methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and its crystalline. WO 2014113616. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XXXIII) | 67664 | 4-chloro-6-methoxyquinolin-7-ol | C10H8ClNO2 | 详情 | 详情 | |
| (XXXVI) | 67667 | 4-methoxybenzyl (1-(hydroxymethyl)cyclopropyl)carbamate | C13H17NO4 | 详情 | 详情 | |
| (XXXIX) | 67671 | 4-methoxybenzyl (1-(((6-methoxy-4-((5-(methylcarbamoyl)naphthalen-2-yl)oxy)quinolin-7-yl)oxy)methyl)cyclopropyl)carbamate | C35H33N3O7 | 详情 | 详情 | |
| (XLV) | 67676 | 4-methoxybenzyl (1-(((4-chloro-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropyl)carbamate | C23H23ClN2O5 | 详情 | 详情 | |
| (XLVI) | 67677 | 1-(((6-methoxy-4-((5-(methylcarbamoyl)naphthalen-2-yl)oxy)quinolin-7-yl)oxy)methyl)cyclopropanecarbonyl azide | C27H23N5O5 | 详情 | 详情 |
Extended Information