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【结 构 式】 
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【分子编号】28314 【品名】N-(4-benzoylphenyl)-N-[2-(diethylamino)ethyl]acetamide 【CA登记号】 |
【 分 子 式 】C21H26N2O2 【 分 子 量 】338.44972 【元素组成】C 74.53% H 7.74% N 8.28% O 9.45% |
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：(IV)The acetylation of 4-aminobenzophenone (I) with acetic anhydride and TEA in dichloromethane gives the acetamide (II), which is N-alkylated with 2-chlorethyl(diethyl)amine (III) by means of KOH in refluxing acetone yielding the disubstituted acetamide (IV). The reaction of the ketonic group of (IV) with benzylphosphonic acid diethyl ester (V) by means of butyllithium and benzenesulfonyl chloride in THF affords the chlorovinyl acetamide (VI), which is finally hydrolyzed with HCl and salified with citric acid to provide the target compound.
| 【1】 Bitonti, A.J. (Aventis Pharmaceuticals, Inc.); Method of using triaryl-ethylene derivs. in the treatment and prevention of osteoporosis. US 5691384; WO 9616646 . |
| 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) | 28307 | (4-aminophenyl)(phenyl)methanone | 1137-41-3 | C13H11NO | 详情 | 详情 |
| (II) | 28313 | N-(4-benzoylphenyl)acetamide | C15H13NO2 | 详情 | 详情 | |
| (III) | 16194 | 2-chloro-N,N-diethyl-1-ethanamine; N-(2-chloroethyl)-N,N-diethylamine | 100-35-6 | C6H14ClN | 详情 | 详情 |
| (IV) | 28314 | N-(4-benzoylphenyl)-N-[2-(diethylamino)ethyl]acetamide | C21H26N2O2 | 详情 | 详情 | |
| (V) | 28315 | diethyl benzylphosphonate | 1080-32-6 | C11H17O3P | 详情 | 详情 |
| (VI) | 28312 | N-[4-[(E)-2-chloro-1,2-diphenylethenyl]phenyl]-N-[2-(diethylamino)ethyl]acetamide | C28H31ClN2O | 详情 | 详情 |
Extended Information