Study Of Docetaxel Synthesis Process

Objective: The synthesis of high purity of docetaxel utilizing 10-deacetyl baccatin III(10-DAB III) which was extracted from the residuary of taxus extraction. Methods: The residuary of taxus extraction was extracted by petroleum ether defatted waste, filtration, and then purified by column chromatography and recrystallization, the highly pure 10-DABIII was obtained; 10-DABIII, the starting material, reacted with Benzyl Chloroformate to form C-7, C-10-type of oxycarbonyl-protected 10-DABIII, and then condensed with (3R,4S)-1- tert-butoxy-carbonyl-3- (1-ethoxy-ethyl oxy)-4-phenylazetidin-2-one, followed by hydrogenolysis to form a 2'-(1 - ethoxy-ethyl oxy)-N-off Benzoyl-N-tert-butyl carbonyl oxygen -10 - deacetyl taxol, and the target molecule was finally obtained by the acid hydrolysis. Results: The target molecule and the intermediate was identified by infrared spectrum, mass spectrometry, NMR structure. Conclusion: The method will benefit from the mild conditions, high yield, the according quality requirements for the injection of medicine and the use of raw materials.