| 摘要 |
The invention relates to a process for preparing paclitaxel or docetaxel from 9-dihydro-13-acetylbaccatin III, the process comprising the steps of: protecting the hydroxy group at the C-7 position of the 9-dihydro-13-acetylbaccatin III to yield a first C-7 protected 9-dihydro-13-acetylbaccatin III derivative; oxidizing the hydroxy group at the C-9 position of the first C-7 protected 9-dihydro-13-acetylbaccatin III derivative to yield a second C-7 protected 13-acetylbaccatin III derivative; cleaving the ester linkage at, and attaching a side chain to, the C-13 position of the second C-7 protected 13-acetylbaccatin III derivative to yield a C-13 protected taxane intermediate; and converting the C-13 protected taxane intermediate to paclitaxel or docetaxel, wherein the step of cleaving the ester linkage at, and attaching a side chain to, the C-13 position of the second C-7 protected 13 -acetylbaccatin III derivative comprises combining the second C-7 protected 13-acetylbaccatin III derivative with both a base and a precursor to the side chain, and wherein the precursor to the side chain is selected from the group consisting of beta-lactams, oxazolidines and oxazolines. This is shown by way of example in the following scheme: (see above scheme) |
