A METHOD FOR PREPARING DOCETAXEL AND NEW INTERMEDIATES FOR PREPARING THE SAME

摘要

PURPOSE: A novel intermediate for preparing docetaxel and a method for preparing the docetaxel using the same are provided to easily remove protection group and simply and economically prepare docetaxel with high yield and purity. CONSTITUTION: A method for preparing docetaxel of chemical formula I comprises: a step of performing coupling reaction of (4S,5R)-4-phenyl-2-trichloromethyl-oxazolidine-5-carboxylic acid of chemical formula VI with 10-deacetyl baccatin III of chemical formula III to obtain 13-[(4S,5R)-4-phenyl-2-trichloromethyl-oxazolidine-5-carbonyl-10-deacethyl baccatin III of chemical formula VII in which 7,10 hydroxy group is protected; a step of reacting the 13-[(4S,5R)-4-phenyl-2-trichloromethyl-oxazolidine-5-carbonyl-10-deacethyl baccatin III in solvent under the presence of acid to remove protection group of phenylisoserine; a step of reacting with di-t-butyl dicarbonate under the presence of base to obtain docetaxel of chemical formula VIII in which 7,10 hydroxy group is protected; and a step of removing 7 and 10 position protection group of the docetaxel under the presence of reaction solvent.