Semi-Synthesis And Quality Standards Research Of Taxol

Taxol is a tetracyclic diterpenoid, because of its unique machan ism of anticancer and highly effective anti-tumor activity, has becom e a preferred drug for the treatment for ovarian cancer, breast cance r and many other kinds of cancer. Taxol is firstly extracted in Taxus brevifolia, however, because the low content in the bark, which is n on-renewable, and the slow growth of yew, makes it unable to meet the needs in clinical application, chemical synthesis has become the mai n way to solve this contradiction. We accomplished taxol starting wit h 10-deacetylbaccinâ…¢(10-DABâ…¢), because 10-DABâ…¢exists in the branche s and leaves, which are renewable, and the content is higher than tax ol, makes semi-synthesis of taxol by 10-DABâ…¢ a very possible way.We taxol starting with 10-DABâ…¢ in four steps, also study the qua lity standard of homemade taxol refer to Chinese pharmacopoeia(2010 v ersion).The semi-synthesis of taxol starting with 10-DABâ…¢ in four steps is established:firstly, C7 and C10 hydroxide radical of 10-DABâ…¢ is pr acetotected with 2,2,2,-trichloroethyl chloroformate and acetylchlori de, then, the side chain is connected with protected 10-DABâ…¢ in the presence of DCC, the aim compound is obtained after eliminating the p rotect group and open side chain ring with HC1/C2H5OH.Studied the quality standard of homemade taxol, including charact er, identification, related substances examination and content determ ination. Also complete two sets of methodology research, the results showed that every item meets the standard.