摘要
A new route for the synthesis of cabazitaxel （Javanta） starting with 10-deacetylbaccatin III was developed. In this new procedure, a mild condition for the methylation of 7-OH was applied, thus the epimerization of 7β-OH under basic conditions was reduced. The total yield of this 6-step synthesis is 20%.
本文报道了一种以10-去乙酰基巴卡丁III为起始原料合成卡巴他赛的新方法。路线中使用了温和的条件对底物7-羟基进行甲醚化,从而避免了7β-羟基在强碱性条件下的差向异构化。该路线共6步,总收率为20%。
基金
NSFC(Grant No.30930108)
MOST(Grant No.2009YZH-LCH03)
