| 摘要 |
<p>Process for preparing 3'-N-substituted taxanes from paclitaxel, in which the following steps are carried out: a) deacetylation of the paclitaxel through the action of a peroxide, without the addition of a base; then b) protection of the free hydroxyl functions, respectively in the 7-, 10- and 2'-position; c) debenzoylation of the amino in the 3'-position, to a primary amino, derived from 10-deacetylbaccatin, of which the hydroxyl functions in the 7-, 10- and 2'-position have previously been protected; d) functionalization of the amino with a suitable radical so as to obtain a 3'-N-substituted taxane of general formula (I) in which X is protective radicals or hydrogen atoms and R is a pharmaceutically active taxane residue; then, where appropriate, e) freeing of the initially protected hydroxyl functions so as to obtain docetaxel.</p> |
