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【结 构 式】 
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【药物名称】RO-63-05631-3 【化学名称】4-Amino-N-[2,6-bis(methylamino)pyridin-4-yl]- benzenesulfonamide 【CA登记号】 【 分 子 式 】C13H17N5O2S 【 分 子 量 】307.37674 |
【开发单位】Roche 【药理作用】PHARMACOLOGICAL TOOLS |
合成路线1
Condensation of 4-acetamidobenzenesulfonyl chloride (I) with 4-amino-2,6-dibromopyridine (II) in pyridine at 60 C afforded sulfonamide (III). The acetamido group was then hydrolyzed in refluxing 1 N NaOH to give (IV). Finally, substitution of both bromine atoms for methylamino groups was carried out by heating with liquid MeNH2 at 160 C in an autoclave.
| 【1】 Wagner, A.; Heitsch, H.; Nolkne, G.; Wirth, K.; Bernard, P. (Aventis SA); Fluoralkyl- and fluoralkoxy-substd. heterocyclic bradykinin antagonists. EP 0796848; JP 1998007656; US 5859025 . |
| 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) | 19362 | 4-(acetamido)benzenesulfonyl chloride; N-acetylsulfanilyl chloride | 121-60-8 | C8H8ClNO3S | 详情 | 详情 |
| (II) | 19363 | 2,6-dibromo-4-pyridinamine; 2,6-dibromo-4-pyridinylamine | C5H4Br2N2 | 详情 | 详情 | |
| (III) | 19364 | N-(4-[[(2,6-dibromo-4-pyridinyl)amino]sulfonyl]phenyl)acetamide | C13H11Br2N3O3S | 详情 | 详情 | |
| (IV) | 19365 | 4-amino-N-(2,6-dibromo-4-pyridinyl)benzenesulfonamide | C11H9Br2N3O2S | 详情 | 详情 |
Extended Information