Chromatographic separation method of paclitaxel and cephalomannin

Abstract

A method for separating paclitaxel cephalomannin and other related compounds by obtaining a staring material that contains paclitaxel and cephalomannin; dissolving the staring material in any one a number of particularly defined solvents such as butly formate and butly acetate to form a mixture; subjecting the mixture to column chromatography to obtain an eluted fraction of pactitaxel and cephalomannin and a residue ; and separately drying the paclitaxel and cephalomannin fractions to obtain separate crystalline forms of paclitaxel and cephalomannin, respectively.

Description

field of invention [0001] The present invention relates to the isolation of paclitaxel and the paclitaxel analogue cephalomannin starting from plant extracts of the genus Taxus or cell cultures thereof. Specifically, cephalomanine was separated from paclitaxel by chromatography on a normal phase silica gel column. Background technique [0002] Paclitaxel, formerly known as Taxol, is a particularly promising anticancer agent. In 1971, Wani et al. isolated it from the bark of Taxus brevifolia (J.Am.Chem.Soc.93, 2325, 1971), and determined it by chemical methods and X-ray crystallographic analysis. Structure. [0003] [0004] Paclitaxel has been approved by the FDA for the treatment of breast and ovarian cancer, and its treatment for lung and rectal cancer is currently in clinical trials (see, for example, W.P. McGuire and E.K. Rowinsky, Paclitaxel in Cancer Therapy, M. Dekker, New York 1995 , pp. 1 to 337). [0005] The main natural source of paclitaxel is the bark of ...

AI Technical Summary

Problems solved by technology

However, these methods have the disadvantage of using toxic reagents such as osmium tetroxide and in any case leading to the destruction and conversion of cephalomannine to its derivatives, which can only be obtained by difficult synthetic methods. Regeneration to cephalomanine

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