| 摘要 |
PCT No. PCT/US95/05427 Sec. 371 Date Nov. 1, 1996 Sec. 102(e) Date Nov. 1, 1996 PCT Filed May 2, 1995 PCT Pub. No. WO95/29919 PCT Pub. Date Nov. 9, 1995The present invention relates to a method for the preparation of camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I') known by the chemical name "7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin", which comprises cyclising the compound of formula (II'), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I') is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer, and/or if desired, converting the resulting compound of formula (I') or a salt thereof into a physiologically acceptable salt or solvate thereof.
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