An Improved Synthesis Of7β,10β-Dimethoxy-10-Deacetoxybaccatin Ⅲ

OBJECTIVE:This paper reported the key intermediate of cabazitaxel,7β,10β-dimethoxy-10-deacetoxybaccatin Ⅲ, was synthesized with a new method.METHOD:At first, the C(7) and C(10) hydroxy of10-deacetoxybaccatin III was selectively protected; and then, the C(13) hydroxyl was protected by an another reagent. After the deprotection of C(7) and C(10) hydroxyl, the methylation was carried on C(7) and C(10). group on13was removed and the key intermediate,7β,10β-dimethoxy-10-deacetoxybaccatin III was obtained after the deprotection of C(13) hydroxyl, which was characterized by MS and1H-NMRRESULTS:7β,10β-Dimethoxy-10-deacetoxybaccatin Ⅲ was synthesized successfully with5steps reactions, with the overall yield of50%.CONCLUSON:The method will benefit from the good yield, mild conditions and convenient operations, which is suitable for industrial production.