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【结 构 式】 
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【药物名称】Actisomide, SC-36602 【化学名称】(±)-4-[2-[Bis(1-methylethyl)amino]ethyl]4,4a,5,6,7,8-hexahydro-1-methyl-4-phenyl-3H-pyrido[1,2-c]pyrimidin-3-one 【CA登记号】96914-39-5 【 分 子 式 】C23H35N3O 【 分 子 量 】369.5549 |
【开发单位】Pfizer (Originator) 【药理作用】Antiarrhythmic Drugs, CARDIOVASCULAR DRUGS |
合成路线1
This compound can be obtained by two related ways: 1) The hydrogenation of 4-(diisopropylamino)-2-phenyl-2-(2-pyridyl)butyramide (I) with H2 over PtO2 in acidic water gives the corresponding piperidine derivative (II), which is acetylated with acetic anhydride to the acetylpiperidine (III). Finally, this compound is cyclized by means of KOH in DMSO. 2) The cyclization of piperidine derivative (II) whith dimethylacetamide dimethyl ketal (IV) at 80 C also yields the final produc
| 【1】 McLaughlin, K.T.; Chorvat, R.J.; Stamm, M.H.; Adelstein, G.W.; Stickney, J.L.; Rydzewski, R.M.; Prodan, K.A.; Frederick, L.G.; Schniepp, H.C.; Synthesis and structure-activity relationships of a new series of antiarrhythmic agents: 4,4-disubstituted hexahydro-3H-pyrido[1,2-c]pyrimidin-3-ones and related compounds. J Med Chem 1985, 28, 9, 1285. |
| 【2】 Adelstein, G.W.; Chorvat, R.J. (Pharmacia Corp.); Pyridopyrimidinones. EP 0104647; US 4560754 . |
| 【3】 Baxter, A.D.; Boyd, E.A.; Price, S.; Guicherit, O.M.; Porter, J.; Rubin, L.E. (Curis, Inc.); Small organic molecule regulators of cell proliferation. US 6613798; US 6683108; WO 0174344 . |
| 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) | 22912 | 4-(diisopropylamino)-2-phenyl-2-(2-pyridinyl)butanamide | 3737-09-5 | C21H29N3O | 详情 | 详情 |
| (II) | 22913 | 4-(diisopropylamino)-2-phenyl-2-(2-piperidinyl)butanamide | C21H35N3O | 详情 | 详情 | |
| (III) | 22914 | 2-(1-acetyl-2-piperidinyl)-4-(diisopropylamino)-2-phenylbutanamide | C23H37N3O2 | 详情 | 详情 | |
| (IV) | 22915 | 1,1-dimethoxy-N,N-dimethyl-1-ethanamine;N,N-dimethylacetamide dimethylacetal; N-(1,1-dimethoxyethyl)-N,N-dimethylamine | 18871-66-4 | C6H15NO2 | 详情 | 详情 |