Synthesis Of Docetaxel And Analogues

As the largest sale of anticancer drugs in the history,paclitaxel is widely used in the treatment of the ovarian cancer,the breast cancer,the lung cancer and the Kaposi’s sarcoma,and it is also studied in the treatment and treatment with other anticancer drugs with more types of tumors.Due to the limited extraction of paclitaxel,semi synthetic paclitaxel drug material is particularly important,which has occupied the total sales of 2/3 in the international anticancer durg,and its sale is still growing.Among them,with its characteristics of high efficiency,low toxicity and broadspectrum anti-cancer,docetaxel has occupied the most sale of the market.This thesis taking 10-DABIII as the starting materials,by protecting it with Troc-Cl,then through the DCC/DMAP catalytic esterification,deprotection and ring opening steps,finally obtained docetaxel.Then on the basis of the small test pilot and optimizing rection conditions,we ultimately determined the production process.At the same time,according to the docetaxel intermediate II produced by the research process and amidation by TEA/DCC catalyzing,a series of new paclitaxel analogues were synthesized and characterized.In addition,in order to improve the water solubility of taxol compounds,we used 2,3,4,6-O-Tetraacetyl-α-D-glucopyranosyl bromide connected with docetaxel and paclitaxel analogues by direct or indirect ways to synthesize a series of new water soluble taxol analogues.These results may lay a foundation for further research on the taxol compounds.This not only has important scientific research value,but also has a wide range of market application prospects.