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 2min时, 目的产物7, 10-di(Trpc)-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.

天津市重大科技攻关项目(NO. 98311811)