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【结 构 式】 
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【药物名称】CPT-154 【化学名称】4(S)-Ethyl-4-hydroxy-11-[(E)-(phenylimino)methyl]-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione 【CA登记号】292620-93-0 【 分 子 式 】C27H21N3O4 【 分 子 量 】451.48612 |
【开发单位】Istituto Nazionale Studio e Cura Tumori (Originator), Sigma-Tau (Originator) 【药理作用】ONCOLYTIC DRUGS, Camptothecins, DNA-Intercalating Drugs |
合成路线1
The title imine derivative was prepared by condensation of the known 7-formylcamptothecin (I) with aniline (II) in the presence of ytterbium triflate and molecular sieves in CH2Cl2.
| 【1】 De Cesare, M.; Pratesi, G.; Carenini, N.; Dallavalle, S.; Penco, S.; Ferrari, A.; Merlini, L.; Zunino, F.; Perego, P.; Novel cytotoxic 7-iminomethyl and 7-aminomethyl derivatives of camptothecin. Bioorg Med Chem Lett 2001, 11, 3, 291. |
| 【2】 Carminati, P.; Penco, S.; Zunino, F.; Merlini, L. (Istituto Nazionale per lo Studio e la Cura dei Tumori; Sigma-Tau Industrie Farmaceutiche Riunite SpA); Camptothecin derivs. having antitumor activity. EP 1044977; WO 0053607 . |
Extended Information