Method for the preparation of baccatin iii and derivatives...

Details Method for the preparation of baccatin iii and derivatives... Method for the preparation of baccatin iii and derivatives...

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) A61K 31/337 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2205745

A method for single step conversion of 10-Deacetylbaccatin III of the general formula Image into baccatin III, which is a superior starting material for an improved semisynthesis of paclitaxel or paclitaxel analogues. 10-Deacetylbaccatin III is selectively acylated to baccatin III and derivatives thereof in high yield with anhydrides (e. g. acetic anhydride), catalysed by Lewis acids. Extremely effective catalysts in this reaction are compounds of the formula ML X wherein M is a rare earth metal and L is a anion, preferably a strong electron withdrawing counterion such as triflate.

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