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【结 构 式】 
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【药物名称】SA-627 【化学名称】N-(2-Bromo-4,6-dimethoxyphenyl)-N-ethyl-N-[6-methyl-4-(4-morpholinyl)-1,3,5-triazin-2-yl]amine methanesulfonate 【CA登记号】 【 分 子 式 】C19H28BrN5O6S 【 分 子 量 】534.43291 |
【开发单位】Bristol-Myers Squibb (Originator) 【药理作用】Antidepressants, Anxiolytics, Mood Disorders, Treatment of, PSYCHOPHARMACOLOGIC DRUGS, CRF Receptor Antagonists |
合成路线1
Treatment of cyanuric chloride (I) with methylmagnesium chloride afforded 2,4-dichloro-6-methyltriazine (II), which was condensed with aniline (III) to produce the anilinotriazine (IV). Subsequent displacement of the remaining chlorine atom of (IV) with morpholine (V) provided (VI). The target compound was then obtained by N-alkylation with iodoethane in the presence of NaH, followed by conversion to the methanesulfonate salt).
| 【1】 Arvanitis, A.G.; Chorvat, R.J.; Gilligan, P.J.; et al.; Non-peptide corticotropin-releasing hormone antago. J Med Chem 1999, 42, 5, 805. |
| 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) | 23813 | 2,4,6-Trichloro-s-triazine; Cyanuric chloride; Trichlorocyanidine; Tricyanogen chloride; 2,4,6-Trichloro-1,3,5-triazine | 108-77-0 | C3Cl3N3 | 详情 | 详情 |
| (II) | 23814 | 2,4-dichloro-6-methyl-1,3,5-triazine | C4H3Cl2N3 | 详情 | 详情 | |
| (III) | 23815 | 2-bromo-4,6-dimethoxyphenylamine; 2-bromo-4,6-dimethoxyaniline | C8H10BrNO2 | 详情 | 详情 | |
| (IV) | 23816 | N-(2-bromo-4,6-dimethoxyphenyl)-N-(4-chloro-6-methyl-1,3,5-triazin-2-yl)amine; N-(2-bromo-4,6-dimethoxyphenyl)-4-chloro-6-methyl-1,3,5-triazin-2-amine | C12H12BrClN4O2 | 详情 | 详情 | |
| (VI) | 23818 | N-(2-bromo-4,6-dimethoxyphenyl)-N-[4-methyl-6-(4-morpholinyl)-1,3,5-triazin-2-yl]amine; N-(2-bromo-4,6-dimethoxyphenyl)-4-methyl-6-(4-morpholinyl)-1,3,5-triazin-2-amine | C16H20BrN5O3 | 详情 | 详情 | |
| (X) | 10388 | Morpholine | 110-91-8 | C4H9NO | 详情 | 详情 |