Patent · US Expired

Preparation of a camptothecin derivative by intramolecular cyclisation

US6063923A · kind A · utility

11Cited by
34References
26Claims
0Family size

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Inventors

Key dates

Filing dateNov 1, 1996
Grant dateMay 16, 2000
Priority date
Expiry dateNov 1, 2016

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D491/04
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The 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.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.