Patent ID: 7358378
Filing Date: 2008-04-15
Classification: A61P,C07D,Y02P

Abstract:
1. A process for the preparation of paclitaxel, the process comprising: (a) protecting the C(7) and the C(10) hydroxy groups of 10-deacetylbaccatin III (10-DAB) by treating 10-DAB with a bridging silicon-based protecting group to form 10-DAB derivative (12); (b) derivatizing 10-DAB derivative (12) to form 10-DAB derivative (17), the derivatization comprising: (c) deprotecting 10-DAB derivative (17) to form paclitaxel; wherein 10-DAB derivative (12), 10-DAB derivative (13), 10-DAB derivative (14), 10-DAB derivative (15), 10-DAB derivative (16), and 10-DAB derivative (17), correspond to Formulae (12), (13), (14), (15), (16), and (17), respectively: the bridging silicon-based protecting group corresponds to Formula (2): the β-lactam side chain precursor corresponds to Formula (3B): G L R X Z is hydrocarbyl, substituted hydrocarbyl, heterocyclo, —[O—Si(Z each Z n is 1 or 2.