【药物名称】Topotecan hydrochloride, E-89/001, NSC-609699, SK&F-S-104864-A, Evotropin, Hycamtin
化学结构式(Chemical Structure):
参考文献No.10756
标题:Water soluble camptothecin analogs
作者:Boehm, J.C.; Johnson, R.K.; Hecht, S.M.; Kingsbury, W.D.; Holden, K.G. (SmithKline Beecham plc)
来源:AU 8826394; EP 0321122; JP 1989186893; US 5004758
合成路线图解说明:

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No.140053
标题:Synthesis of water soluble (aminoalkyl) camptothecin analogues: Inhibition of topoisomerase I and antitumor activity
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.
来源:J Med Chem 1991,34(1),98-107
合成路线图解说明:

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No.298942
标题:Topotecan Hydrochloride
作者:Casta馿r, J.; Spiridonidis, C.H.
来源:Drugs Fut 1995,20(5),483
合成路线图解说明:

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.

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