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【结 构 式】 
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【分子编号】16220 【品名】methyl 2-[3-(3-[[6-(benzyloxy)-3-ethyl-4'-fluoro[1,1'-biphenyl]-4-yl]oxy]propoxy)-2-propylphenoxy]benzoate 【CA登记号】 |
【 分 子 式 】C41H41FO6 【 分 子 量 】648.7713432 【元素组成】C 75.91% H 6.37% F 2.93% O 14.8% |
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：(XIII)The final coupling of fragments (VI) and (X) to give (XIII) is shown in Scheme 19757001c, and is accomplished in the presence of potassium carbonate in N,N-dimethylformamide. The final deprotection sequence is effected by hydrogenolysis of the benzyl ether followed by hydrolysis of the resulting ester to provide LY293111 as the sodium salt.
| 【1】 Schmittling, E.A.; Sawyer, J.S.; Synthesis of diaryl ethers, diaryl thioethers, and diaryl amines mediated by potassium fluoride-alumina and 18-crown-6. J Org Chem 1993, 58, 3229-30. |
| 【2】 Sawyer, J.S.; LY-293111 Sodium. Drugs Fut 1996, 21, 6, 610. |
| 【3】 Sawyer, J.S.; Bach, N.J.; Baker, S.R.; et al.; Synthetic and structure/activity studies on acid-substituted 2-arylphenols: The discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5-hydroxyphenoxy]propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist. J Med Chem 1995, 38, 22, 4411-32. |
| 【4】 Sawyer, J.S.; Baldwin, R.F.; Sofia, M.J.; et al.; Biphenylyl-substituted xanthones: Highly potent leukotriene B4 receptor antagonists. J Med Chem 1993, 36, 24, 3982-4. |
| 【5】 Sawyer, J.S.; Baldwin, R.F.; Saussy, D.L. Jr.; Froelich, L.L.; Jackson, W.T.; Diaryl ether/carboxylic acid derivatives of LY255283: Receptor antagonists of leukotriene B4. Bioorg Med Chem Lett 1993, 3, 10, 1985-90. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (VI) | 16213 | benzyl 5-ethyl-4'-fluoro-4-(3-iodopropoxy)[1,1'-biphenyl]-2-yl ether; 2-(benzyloxy)-5-ethyl-4'-fluoro-4-(3-iodopropoxy)-1,1'-biphenyl | C24H24FIO2 | 详情 | 详情 | |
| (X) | 16217 | methyl 2-(3-hydroxy-2-propylphenoxy)benzoate | C17H18O4 | 详情 | 详情 | |
| (XIII) | 16220 | methyl 2-[3-(3-[[6-(benzyloxy)-3-ethyl-4'-fluoro[1,1'-biphenyl]-4-yl]oxy]propoxy)-2-propylphenoxy]benzoate | C41H41FO6 | 详情 | 详情 |
Extended Information