CPT-154
Chemical Name: 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; 7-(Phenyliminomethyl)camptothecin
CAS No. 292620-93-0
项目整合开发状态: Preclinical
项目研究机构: Istituto Nazionale Studio e Cura Tumori (Originator), Sigma-Tau (Originator)
合成路线:Radical hydroxymethylation of camptothecin (I) by means of MeOH in the presence of H2O2 and FeSO4 provided (II).Subsequent heating of alcohol (II) in acetic acid gave rise to 7-formylcamptothecine (III).Finally,condensation of aldehyde (III) with O-t-butylhydroxylamine afforded the corresponding oxime.
合成路线: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.
📌 参考资料/链接：
参考文献标题:Camptothecin derivs.having antitumor activity
文献作者:Carminati,P.; Penco,S.; Zunino,F.; Merlini,L.(Istituto Nazionale per lo Studio e la Cura dei Tumori; Sigma-Tau Industrie Farmaceutiche Riunite SpA)
参考来源:EP 1044977; WO 0053607
📄 详细内容
合成路线: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.
参考文献标题:Novel cytotoxic 7-iminomethyl and 7-aminomethyl derivatives of camptothecin
文献作者:Dallavalle,S.; Ferrari,A.; Merlini,L.; Penco,S.; Carenini,N.; De Cesare,M.; Perego,P.; Pratesi,G.; Zunino,F.
参考来源:Bioorg Med Chem Lett 2001,11(3),291