abstract |
PURPOSE: Provided is a manufacturing method of paclitaxel of the formula (1). Further, novel intermediates used for manufacturing paclitaxel and their manufacturing methods are provided. CONSTITUTION: Paclitaxel is represented by the formula (1) wherein, Ph is phenyl, Ac is acetyl, and Bz is benzoyl. The intermediate used for manufacturing paclitaxel is provided by reacting a novel oxazoline derivative of the formula (2a) or its salt, and (2R,3S)-phenylisoserine derivative of the formula (10) with a compound of the formula (11), in the solvent, in the presence of acid catalyst. In the formulae, X is halogen; R is hydrogen or C1-C3 of alkyl; and R5, R6, and R7 represent individually C1-C4 of alkyl or phenylalkyl, or R5 and R6 form 4-7 membered ring of cyclic chain together. |