PROCESS FOR PREPARATION OF PACLITAXEL

摘要

PURPOSE: Provided is a novel preparation method of paclitaxel represented by the formula (1) (wherein R is t-butylcarbonyl or benzoyl and R1 is trihaloacetyl). Therefore, paclitaxel is simply synthesized under very mild condition. CONSTITUTION: A preparation method of paclitaxel is composed of the following steps of: (a) coupling oxazolidine dimer derivative represented by the general formula (2) or the salt thereof with 7-trihaloacetyl-bacatine 3 represented by the formula (3 in the presence of condensation agent) in solvent, to produce oxazolidine branched-containing taxan dimer represented by the formula (4); (b) opening the oxazolidine ring in the presence of acid in solvent and additionally reacting with benzoylchloride if R is t-butoxycarbonyl, in the presence of base, to produce 7-trihaloacetylpaclitaxel represented by the formula (5); and (c) eliminating trihaloacetyl of 7-position in solvent with ammonia or salt of ammonia and weak acid.