Paclitaxel preparation method

Abstract

The invention provides a paclitaxel preparation method, wherein a raw material 7-xylosyl-10-deacetyltaxol (10DAXT) is subjected to pretreatment conversion to obtain a paclitaxel mixture (the pretreatment steps comprise ozone oxidation, a C-7 site xylosyl removing reaction, a C-10 site acetyl introduction reaction, and the like), and the obtained paclitaxel mixture is subjected to column chromatography, recrystallization and other steps to obtain the paclitaxel pure product. With the method, the paclitaxel mixture derived from the 10DAXT can be effectively separated; and efficient, inexpensive and environmental protection paclitaxel preparation can be achieved, and an effective path suitable for industrial production is provided for complete yew resource utilization.

Description

technical field [0001] The invention belongs to the field of pharmaceutical industry, and specifically relates to a method for separating high-purity paclitaxel from 10DAXT conversion products by utilizing high-efficiency column chromatography and crystallization technology. Background technique [0002] Paclitaxel (1) is a kind of diterpene compound, which is widely used in the treatment of various tumors as a first-line clinical drug. At present, the main ways to produce paclitaxel are: ⑴ directly extracting paclitaxel from Taxus plants; 2), and then use chemical methods to semi-synthesize paclitaxel. [0003] [0004] [0005] Except 10DAB, in the branches and leaves of several yew varieties (Yunnan, South, Chinese yew) widely planted in my country, there is also another kind of compound with paclitaxel mother nucleus structure in a large number, i.e. 10-deacetyl- 7-xylose paclitaxel (10DAXT) (3), its content can reach 1‰ of plant dry weight, which is 5-10 times tha...

AI Technical Summary

Problems solved by technology

Since 10DAXT from plant sources is usually accompanied by other kinds of taxane xyloside compounds, such as 10-deacetyl-7-xylose cephalomannine (10DAXC), 10-deacetyl-7-xylose paclitaxel C ( 10DAXTC), the two will participate in the reaction together in the conversion process of 10DAXT, and finally produce cephalomannine and paclitaxel C. These compounds are very similar to paclitaxel in structure, and it is difficult to separate them by ordinary methods; in addition, due to the use of new raw materials and new processes, The raw materials and each step will inevitably introduce many impurities that have not appeared in the existing process. Therefore, efficient separation methods must be used to remove these impurities and ensure that the product meets the pharmacopoeia standards of various countries.

Images