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【结 构 式】 
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【分子编号】18879 【品名】3,4-dihydro-1H-1-benzazepine-2,5-dione 【CA登记号】 |
【 分 子 式 】C10H9NO2 【 分 子 量 】175.187 【元素组成】C 68.56% H 5.18% N 8% O 18.27% |
与该中间体有关的原料药合成路线共 2 条
合成路线1
该中间体在本合成路线中的序号：(I)Benzazepinedione (I) was condensed with propenone (II) in the presence of a catalytic amount of KOH in ethanol to furnish a diasteromeric mixture of the Michael adducts (III). This mixture was then cyclized and oxidized by means of ammonium ferric sulfate and ammonium acetate in refluxing acetic acid to provide the desired pyridobenzazepinone.
| 【1】 Link, A.; Kunick, C.; d-Fused[1]benzazepines with selective in vitro antitumor activity: Synthesis and structure-activity relationships. J Med Chem 1998, 41, 8, 1299. |
合成路线2
该中间体在本合成路线中的序号：(II)The condensation of p-nitrophenylhydrazine (I) with benzazepinedione (II) in AcOH produced hydrazone (III). Subsequent Fischer indole synthesis employing (III) and H2SO4 furnished the title indolobenzazepinone.
| 【1】 Schultz, C.; Zaharevitz, D.W.; Mejer, L.; Gussio, R.; Leost, M.; Sausville, E.A.; Kunick, C.; Link, A.; Paullones, a series of cyclin-dependent kinase inhibitors: Synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J Med Chem 1999, 42, 15, 2909. |
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