| 摘要 |
<p>PURPOSE: A method for preparing a docetaxel and a novel intermediate for preparing the docetaxel are provided to prepare the docetaxel of high purity and high yield. CONSTITUTION: A method for preparing a docetaxel of chemical formula I comprises: a step of performing coupling reaction of (4S,5R)-2-dichloromethyl-2-methyl-4-phenyl-oxazolidine-5-carboxylic acid trialkylamine salt of chemical formula VI with 7,10-bis(aryloxycarbonyl)-10-deaetylbaccatin III of chemical formula III to obtain 7,10-bis(aryloxycarbonyl)-13-((4S,5R)-2-dichloromethyl-2-methyl-4-phenyl-oxazolidine-5-carbonyl)-10-deacetylbaccatin III of chemical formula VII; a step of reacting the compound of chemical formula VII and removing phenylisoserine protection group; a step of reacting with di-t-butyl dicarbonate under the presence of base to obtain 7,10-bis(aryloxycarbonyl)-docetaxel of chemical formula VIII; and a step of reacting 7,10-bis(aryloxycarbonyl)-docetaxel under the presence of reaction solvent.</p> |
