Procedures for the preparation of carbazitaxel involving silylation in C (7) -OH and C (13) -OH or only silylation in C (7) -OH

摘要

A process for the preparation of cabazitaxel (I), comprising the steps of: a) treating 10-deacetylbaccatin of formula (III) ** Formula ** with a silylating agent in the presence of a base and a suitable organic solvent for 1 to 10 hours to obtain a compound of the formula (IV); ** Formula ** b) methylating the compound of the formula (IV) in the presence of a base and a methylating agent to obtain the compound of the formula (V); and ** Formula ** c) deprotecting the silyl group of the compound of formula (V) in the presence of a suitable organic solvent and a base to obtain the compound of formula (VI); ** Formula ** d) methylating the compound of formula (VI) in the presence of a suitable organic solvent and a base to give a compound of formula (II); and ** Formula ** e) converting the compound of formula II to cabazitaxel (I).