Method for preparing cabazitaxel from 10-deacetylbaccatin III in high yield, and novel intermediate therefor

摘要

The present invention relates to a novel method for preparing cabazitaxel from 10-deacetylbaccatin III, and a novel intermediate therefor, and more specifically, to: a method which allows cabazitaxel to be more easily prepared in a high yield and in a high purity within a short time compared with a conventional method by preparing cabazitaxel via a novel intermediate using 10-deacetylbaccatin III as a starting material, and thus is suitable for industrial mass production; and a novel intermediate therefor.

主权项

1. A method for preparing cabazitaxel comprising the steps of:
1) reacting 10-deacetylbaccatin III of Chemical Formula 2 with a silylating agent to obtain an intermediate of Chemical Formula 3 in which hydroxy group at the 7 position is protected by a silylated radical; 2) methylating hydroxy group at the 10 position of the intermediate of Chemical Formula 3 to obtain an intermediate of Chemical Formula 4; 3) deprotecting hydroxy group at the 7 position of the intermediate of Chemical Formula 4 to obtain an intermediate of Chemical Formula 5; 4) methylating hydroxy group at the 7 position of the intermediate of Chemical Formula 5 to obtain an intermediate of Chemical Formula 6; 5) esterifying hydroxy group at the 13 position of the intermediate of Chemical Formula 6 in the presence of oxazolidine acid derivative of Chemical Formula 8 to obtain an intermediate of Chemical Formula 7; and 6) treating the intermediate of Chemical Formula 7 with an acid to obtain cabazitaxel of Chemical Formula 1: wherein Ac represents acetyl group; Me represents methyl group; Ph represents phenyl group; and M represents a silylated radical.