【结 构 式】 |
【药物名称】 【化学名称】1-(2-Amino-4-methoxyphenyl)-1-(3,4,5-trimethoxyphenyl)methanone 【CA登记号】 【 分 子 式 】C17H19NO5 【 分 子 量 】317.34468 |
【开发单位】National Health Research Institutes (Originator) 【药理作用】Oncolytic Drugs, Antimitotic Drugs, Microtubule-Stabilizing Agents |
合成路线1
Treatment of 3,4,5-trimethoxybromobenzene (I) with Mg in THF produces the corresponding Grignard reagent (II), which is condensed with 4-methoxy-2-nitrobenzaldehyde (III) to furnish the benzhydrol derivative (IV). Oxidation of benzhydrol (IV) by means of pyridinium dichromate leads to benzophenone (V). The nitro group of (V) is then reduced to the corresponding amine employing iron powder in AcOH.
【1】 Liou, J.-P.; et al.; Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents. J Med Chem 2002, 45, 12, 2556. |
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) | 64554 | 4-bromo-2,6-dimethoxyphenyl methyl ether; 5-bromo-1,2,3-trimethoxybenzene | C9H11BrO3 | 详情 | 详情 | |
(II) | 32378 | bromo(3,4,5-trimethoxyphenyl)magnesium | C9H11BrMgO3 | 详情 | 详情 | |
(III) | 64555 | 4-methoxy-2-nitrobenzaldehyde | C8H7NO4 | 详情 | 详情 | |
(IV) | 64556 | (4-methoxy-2-nitrophenyl)(3,4,5-trimethoxyphenyl)methanol | C17H19NO7 | 详情 | 详情 | |
(V) | 64557 | (4-methoxy-2-nitrophenyl)(3,4,5-trimethoxyphenyl)methanone | C17H17NO7 | 详情 | 详情 |
Extended Information