10-去乙酰基巴卡亭Ⅲ羟基保护反应过程的研究

Studies on the Protection of Hydroxy Groups in 10-deacetyl Baccatin III

对半合成紫杉醇类化合物的关键步骤 １０－去乙酰基巴卡亭 Ⅲ（１０－ＤＡＢ）的羟基保护反应进行了研究。结果表明，利用氯甲酸（２，２，２－三氯）乙酯作为羟基保护基，获得７。１０－二（三氯乙氧基）－１０一去乙酰基巴卡亭Ⅲ［７，１０－ｄｉ（Ｔｒｏｃ）－１０－ＤＡＢ］的反应为连串反应，受反应时间和温度影响较大。当反应温度为 ８０℃，反应时间为 ２ ｍｉｎ时，目的产物 ７，１０－ｄｉ（Ｔｒｏｃ）－１０－ＤＡＢ的反应选择性最好。

The use of 2, 2, 2-trichloroethyl chloroformate as the hydroxy protecting group of 10deacetyl baccatinⅢ was studied to give 7, 10-di (2, 2, 2-trichloroethyloxycarbonyl)-10- baccatinⅢ, the key intermediate for the semisynthesis of taxanes. Result of the study showed that it is a consecutive reaction which could be significantly effected by reaction conditions of temperature and time. It was found that at 80C for 2 min the selectivity of 7, 10-di(2, 2, 2-trichloroethyloxycarbonyl)-10- baccatin Ⅲ is at its best.