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【结 构 式】 
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【药物名称】HMR-1402 【化学名称】5-Chloro-2-methoxy-N-[2-[4-(2-methoxyethoxy)-3-(3-methylthioureidosulfonyl)phenyl]ethyl]benzamide 【CA登记号】181272-10-6 【 分 子 式 】C21H25ClN3NaO6S2 【 分 子 量 】538.0207 |
【开发单位】Aventis Pharma (Originator) 【药理作用】Antiarrhythmic Drugs, CARDIOVASCULAR DRUGS, K(ATP) Channel Blockers |
合成路线1
Amine (I) was converted into amide (III) by condensation with 5-chloro-2-methoxybenzoyl chloride (II). Chlorosulfonation of (III), followed by reaction with ammonia, furnished the corresponding sulfonamide (IV). The required sulfonyl thiourea function was generated by condensation of sulfonamide (IV) with methyl isothiocyanate in the presence of NaH. The title compound was finally isolated as the corresponding sodium salt.
| 【1】 Englert, H.C.; Gerlach, U.; Mania, D.; Gögelein, H.; Kaiser, J. (Aventis SA); Substd. benzenesulfonylureas and -thioureas, process for their preparation, their use as medicament or diagnostic agent, as well as medicaments containing them. DE 19505397; EP 0727416; JP 1996245554; US 5652268 . |
| 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) | 44239 | 4-(2-methoxyethoxy)phenethylamine; 2-[4-(2-methoxyethoxy)phenyl]-1-ethanamine | C11H17NO2 | 详情 | 详情 | |
| (II) | 44240 | 5-chloro-2-methoxybenzoyl chloride | C8H6Cl2O2 | 详情 | 详情 | |
| (III) | 44241 | 5-chloro-2-methoxy-N-[4-(2-methoxyethoxy)phenethyl]benzamide | C19H22ClNO4 | 详情 | 详情 | |
| (IV) | 44242 | N-[3-(aminosulfonyl)-4-(2-methoxyethoxy)phenethyl]-5-chloro-2-methoxybenzamide | C19H23ClN2O6S | 详情 | 详情 |
Extended Information