机构地区: 广东海洋大学理学院应用化学系
出 处: 《化学研究》 2008年第2期1-4,共4页
摘 要: 以市场可购得的(2R,3S)-苯基异丝氨酸盐酸盐为起始原料,通过在甲醇的氯化亚砜溶液中进行酯化反应,及随后对氨基进行苯甲酰化,氨基羟基的环化保护,最后对其酯进行水解,合成得到保护的预酯化的紫杉醇侧链.整个过程无需柱层析操作,适于工业化生产.为制备保护的预酯化紫杉醇侧链提供了一种有效而又实用的合成方法. Starting from the commercially tected, esterification-ready paclitaxel side lisoserine talization hydrochloride with s and hydrolysis. The available (2R, 3S)-phenylisoserine hydrochloride, the proulfurous dichloride in methanol, following benzoylation, cyclic N, O-acewhole process was purified without column chromatography and suitable for large scale production. A practical and efficient synthesis of the protected, esterification-ready paclitaxel side chain was established.