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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。
Hydroxylation of 10-deacetylbaccatin III (10-DAB), the key step of semisynthetic paclitaxel, was investigated. The results showed that 7.10-bis (trichloroethoxy) -10-deacetylbaccatin III [7, 10 -di (Troc) -10-DAB] is a series of reactions, which are greatly affected by reaction time and temperature. When the reaction temperature was 80 ℃ and the reaction time was 2 min, the reaction product of 7,10-di (Troc) -10-DAB was the best.