Process for coproducing high purity taxol cephalomtanine, and 10-deacetyl Bakating III

Abstract

The present invention provides coproducting process of high purity taxol, 10-deacetyl Bakating III and cephalomtaine from alcohol extractive of leaf, bark or branch of taxad. The copreoducing process includes dissolution of the alcohol extractive with butyl acetate, sodium bicarbonate solution reverse extraction to eliminate impurity, decompression evaporation of the organic phase to eliminate solvent, acetonitrile dissolution of the residuum, cooling crystallization to obtain 10-deacetyl Bakating III, purifying crystallization mother liquid through inversed phase chromatography with polymer stuffing as fixed phase to obtain cephalomtanine and taxol, freezing crystallization to separate the effective components from the inversed phase chromatography eluent and forward phase chromatography with silica gel stuffing as fixed phase to obtain taxol product with purity as high as 99.6%.

Description

technical field [0001] The present invention relates to the joint preparation of taxol, cephalmannine and 10-deacetylbaccatin with a purity of ≥99.5% by using leaves, bark and branches of yew plants and their variants as raw materials III (10-deacetyl baccatin III) method. Background technique [0002] Paclitaxel and some semi-synthetic taxane derivatives such as Taxotere have become a class of effective anticancer drugs. 10-Deacetylbaccatin III and cephalomannine are the main raw materials of semi-synthetic taxane drugs, and together with paclitaxel, they exist in the leaves, bark, and branches of many Taxaceae plants, which are required by the modern pharmaceutical industry The purity of the paclitaxel bulk drug should reach ≥99.5%, and the purity of cephalomannine and 10-deacetylbaccatin III should also reach ≥98%. [0003] The reported method for extracting paclitaxel from various taxus plants requires a cumbersome separation process, such as the separation method disc...

AI Technical Summary

Problems solved by technology

But when preparing extractum by this method, still extract the methanol extract of yew bark or leaf with dichloromethane (or chloroform), at this stage 10-deacetylbaccatin III will be lost in the aqueous phase, causing Product loss

This method reveals that when the active ingredients such as paclitaxel are separated from the eluent, the method of concentration and drying is inconvenient in industrial operation, and it is easy to cause the degradation of paclitaxel products.

In the application of this method, it was found that a large amount of degradation products would be produced in the extracts of bark or leaves stored for a long time, and the retention value of these degradation products was similar to that of paclitaxel, which interfered with the preparation of paclitaxel by reversed-phase chromatography. affect the purity of the product

So far, there is no report on the preparation of pure cephalomannine