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【结 构 式】 
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【药物名称】BR-227 【化学名称】N-[2,4-Dibromo-6-(N-cyclohexyl-N-methylaminomethyl)phenyl]-4-hydroxy-3-methoxybenzamide 【CA登记号】84461-99-4 【 分 子 式 】C22H26Br2N2O3 【 分 子 量 】526.27212 |
【开发单位】Abbott (Originator) 【药理作用】Expectorants, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders |
合成路线1
The acylation of 2,4-dibromo-6-(N-cyclohexyl-N-methylaminomethyl)aniline (I) with 4-(ethoxycarbonyloxy)-3-methoxybenzoyl chloride (II) in CHCl3 gives the corresponding amide (III), which is deprotected by a treatment with aqueous 20% NaOH.
| 【1】 Koshinaka, E.; Ogawa, N.; Kurata, S.; Yamagashi, K.; Kato, I. (Hokuriku Seiyaku Co., Ltd.); 2-Benzoylamino substituted benzylamine derivative and a process for preparation thereof. DE 3209970; EP 0061157; ES 510608 . |
| 【2】 Chu, S.S.; BR-227. Drugs Fut 1985, 10, 3, 186. |
| 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) | 28174 | 2,4-dibromo-6-[[cyclohexyl(methyl)amino]methyl]aniline | C14H20Br2N2 | 详情 | 详情 | |
| (II) | 29039 | 4-(chlorocarbonyl)-2-methoxyphenyl ethyl carbonate | C11H11ClO5 | 详情 | 详情 | |
| (III) | 29040 | 4-[(2,4-dibromo-6-[[cyclohexyl(methyl)amino]methyl]anilino)carbonyl]-2-methoxyphenyl ethyl carbonate | C25H30Br2N2O5 | 详情 | 详情 |
Extended Information