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项目整合精选>>>Topotecan hydrochloride, E-89/001, NSC-609699, SK&F-S-104864-A, Evotropin, Hycamtin
Topotecan hydrochloride, E-89/001, NSC-609699, SK&F-S-104864-A, Evotropin, Hycamtin
盐酸拓扑替康 托泊替康醋酸盐 拓扑替康Chemical Name: (S)-10-Dimethylaminomethyl-9-hydroxycamptothecin monohydrochloride; (4S)-10-(Dimethylaminomethyl)-4-ethyl-4,9-dihydroxy-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione monohydrochloride
CAS No. 119413-54-6, 123948-88-9 (acetate salt), 123948-87-8 (free base)
项目整合开发状态: Launched-1996
项目研究机构: GlaxoSmithKline (Originator), Nippon Kayaku (Not Determined), National Cancer Institute (Codevelopment)
合成路线:The reduction of camptothecin (I) with H2 over PtO2 in acetic acid,followed by oxidative acylation with lead tetraacetate and acetic acid and hydrolysis with acetic acid/water gives 9-hydroxycamptothecin (II),which is then treated with formaldehyde and dimethylamine in acetic acid.The hydrochloride salt is prepared by treatment of the acetic acid solution with diluted HCl.
📌 参考资料/链接：
参考文献标题:Water soluble camptothecin analogs
文献作者:Boehm,J.C.; Johnson,R.K.; Hecht,S.M.; Kingsbury,W.D.; Holden,K.G.(SmithKline Beecham plc)
参考来源:AU 8826394; EP 0321122; JP 1989186893; US 5004758
📄 详细内容
合成路线:The reduction of camptothecin (I) with H2 over PtO2 in acetic acid,followed by oxidative acylation with lead tetraacetate and acetic acid and hydrolysis with acetic acid/water gives 9-hydroxycamptothecin (II),which is then treated with formaldehyde and dimethylamine in acetic acid.The hydrochloride salt is prepared by treatment of the acetic acid solution with diluted HCl.
参考文献标题:Synthesis of water soluble (aminoalkyl) camptothecin analogues: Inhibition of topoisomerase I and antitumor activity
文献作者:Kingsbury,W.D.; Boehm,J.C.; Jakas,D.R.; Holden,K.G.; Hecht,S.M.; Gallagher,G.; Caranfa,M.J.; McCabe,F.L.; Faucette,L.F.; Johnson,R.K.; et al.
参考来源:J Med Chem 1991,34(1),98-107
合成路线:The reduction of camptothecin (I) with H2 over PtO2 in acetic acid,followed by oxidative acylation with lead tetraacetate and acetic acid and hydrolysis with acetic acid/water gives 9-hydroxycamptothecin (II),which is then treated with formaldehyde and dimethylamine in acetic acid.The hydrochloride salt is prepared by treatment of the acetic acid solution with diluted HCl.
参考文献标题:Topotecan Hydrochloride
文献作者:Castar,J.; Spiridonidis,C.H.
参考来源:Drugs Fut 1995,20(5),483