Study On The Synthesis Process And Activity Of Paclitaxel And Its Derivatives

Paclitaxel has been favored for more than 20 years because of its unique mechanism of action.Research on its derivatives is also extremely popular.Researchers have done a lot of structural transformation and derivative design around it,of which Cabazitaxel is the most representative.The sales volume of paclitaxel raw materials is also growing continuously,showing that its influence is still huge.Based on the reference,this subject has studied the semisynthesis and technology of paclitaxel,using 10-DABIII as the starting material,selectively protecting the hydroxyl group in the 10 position,and hydroxyl group in 7 position using Troc-Cl,Condensation of the oxazolidine side chain with the mother nucleus,ring opening and deprotection of the condensation product,finally we finished paclitaxel.After the completion of the pilot test,conditions were optimized and the synthetic route was finally.The final semi-synthetic taxol industrial production line was established through process amplification and further optimization of conditions,finally,we accomplished the production of taxol about 800 g scale.we seeked a route that is easy to industrialize and solve the production problem for the enterprise.The character of the route is that mild conditions,high yield,easy to obtain raw materials and easy operation.Paclitaxel has disadvantages such as poor water solubility and multi-drug resistance of paclitaxel and so on,which limits its application.In order to overcome these shortcomings and seek for derivatives that are more active than paclitaxel.Nine kinds of new paclitaxel derivatives were designed and synthesized according to relevant literature.These compounds were modified from the 3?N position group.And these compounds were screened for anti-tumor activity,and the activity results were not satisfactory.Compared with paclitaxel,the activity was much lower,we will also study the anti-tumor activity of these compounds in future.The structural modification of paclitaxel is still a hot topic,and this subject is only a preliminary exploration of the structural modification of paclitaxel.