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【结 构 式】 
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【药物名称】 【化学名称】N-[2-[4-(Dimethylamino)benzamido]-4-hydroxyphenyl]-4-methoxybenzamide 【CA登记号】219491-20-0 【 分 子 式 】C23H23N3O4 【 分 子 量 】405.45746 |
【开发单位】Lilly (Originator) 【药理作用】Anticoagulants, Coagulation Disorders Therapy, HEMATOLOGIC DRUGS, Coagulation Factor Xa Inhibitors |
合成路线1
Treatment of 4-(dimethylamino)benzoic acid (I) with thionyl chloride produced the corresponding acid chloride (II). Subsequent coupling of (II) with 4-tert-butyldimethylsilyloxy-N1-(4-methoxybenzoyl)-1,2-benzenediamine (III) yielded the bisamide (IV). Finally, desilylation of (IV) in the presence of HCl in aqueous THF afforded the title phenol compound.
| 【1】 Herron, D.K.; et al.; 1,2-Dibenzamidobenzene inhibitors of human factor Xa. J Med Chem 2000, 43, 5, 859. |
| 【2】 Antithrombotic agents. WO 9900121 . |
| 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) | 39987 | 4-(dimethylamino)benzoic acid | 619-84-1 | C9H11NO2 | 详情 | 详情 |
| (II) | 39988 | 4-(dimethylamino)benzoyl chloride | 4755-50-4 | C9H10ClNO | 详情 | 详情 |
| (III) | 39989 | N-(2-amino-4-[[tert-butyl(dimethyl)silyl]oxy]phenyl)-4-methoxybenzamide | C20H28N2O3Si | 详情 | 详情 | |
| (IV) | 39990 | N-[5-[[tert-butyl(dimethyl)silyl]oxy]-2-[(4-methoxybenzoyl)amino]phenyl]-4-(dimethylamino)benzamide | C29H37N3O4Si | 详情 | 详情 |
Extended Information