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【结 构 式】

【药物名称】CRL-8276

【化学名称】12-Methoxy-8H-benzo[b]pyrido[4,3,2-de]-1,7-phenanthrolin-8-one

【CA登记号】

【 分 子 式 】C19H11N3O2

【 分 子 量 】313.31842

【开发单位】Lafon (Originator)

【药理作用】ONCOLYTIC DRUGS

合成路线1

The cyclization of dimethylhydrazone (I) with 4-methoxyquinoline-5,8-dione (II) in refluxing acetic anhydride gives the pyridoquinolinedione (III), which is finally cyclized to the target pentacyclic ketone by means of TFA in refluxing dichloromethane.

1 Bastide, J.; Darro, F.; Bontemps-Subielos, N.; Frydman, A.; Decaestecker, C.; Delfourne, E.; Kiss, R.; Synthesis and characterization of the antitumor activities of analogues of meridine, a marine pyridoacridine alkaloid. J Med Chem 2001, 44, 20, 3275.
2 Kiss, R.; Bontemps-Subielos, N.; Frydman, A.; Darro, F.; Bastide, J.; Deflourne, E. (Laboratoires L. Lafon); Pharmaceutical compsn. based on polyaromatic cpds.. FR 2790954; WO 0055160 .
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) 48817 N-(2-[(E)-3-[(E)-2,2-dimethylhydrazono]-1-propenyl]phenyl)-2,2,2-trifluoroacetamide C13H14F3N3O 详情 详情
(II) 48819 4-methoxy-5,8-quinolinedione C10H7NO3 详情 详情
(III) 52020 2,2,2-trifluoro-N-[2-(6-methoxy-5,10-dioxo-5,10-dihydropyrido[3,2-g]quinolin-4-yl)phenyl]acetamide C21H12F3N3O4 详情 详情
Extended Information