Preparation of taxanes from 9-dihydro-13-acetylbaccatin III
AssigneeAccord Healthcare Ltd.
InventorsGaetan Caron, Mettilda Lourdusamy
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Abstract
The present invention relates to a new process for the preparation of 9-dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9-dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7-position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II.
Claims21
A process for the preparation of 9-dihydro-10-deacetylbaccatin III
- which comprises the step of reacting 9-dihydro-13-acetylbaccatin III having the formula:
- with a deacetylating agent in absence of a solvent to concomitantly deacetylate 10- and 13- positions and produce 9-dihydro-10-deacetylbaccatin III.
Dependencies are inferred from the claim text.