卡巴他赛一种手性异构体杂质的合成

Synthesis of Chiral Isomer Impurity in Cabazitaxel

本文介绍了卡巴他赛原料药的一种手性异构体杂质(2α,5β,7β,10β,13α)-4-乙酰氧基-2-苯甲酰氧基-5,20-环氧基-1-羟基-7,10-二甲氧基-9-氧代-11-紫杉烯-13-基-(2R,3R)-3-叔丁氧基羰基氨基-2-羟基-3-苯基丙酸酯的丙酮化合物的合成,该合成路线原料易得,反应条件温和,选择性高,操作简单。该异构体HPLC纯度超过98%,其结构得到NMR、MS确证,可以作为卡巴他赛原料药的质量控制的杂质对照品。

This report maily paied attention on the synthesis of one chiral isomer impurity of Cabazitaxel： （2ct, 513, 713, 1013, 13α）-4-acetoxy-13-（{（2R,3R）-3-[（tertbutoxycarbonyl）amino]-2-hydroxy-3-phenylpropanpyl}oxy）-1-hydroxy-7,-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate-propan-2-one（1 ： 1）. The materials are easy to get, the condition is modest, the selectivity is high and the operation is simple. The structures of target compounds were confirmed by NMR and MS, and their purities were higher than 98 % （by HPLC）. These compounds can be used as the reference substances of the impurities in the quality control of Cabazitaxel.