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第 6 期 雷高乙,等: 酶促酯化拆分-化学消旋串联法制备(S)-布洛芬 ·1217·
时,e.e.值接近于 0,说明(R)-布洛芬已经完全消旋。 3 结论
在环己烷中,利用 CALB 的对映选择性酯化反
应拆分(±)-布洛芬,48 h 拆分效果达到最好,e.e.值
为 100%,(S)-布洛芬收率为 56%;然后,将(S)-布
洛芬分离,将生成的(R)-布洛芬异丁酯水解为(R)-布
洛芬;再以二甲基亚砜为反应介质,利用二异丙基
氨基锂催化(R)-布洛芬的外消旋反应,2 h 消旋完全,
e.e.值为 0;最后,对选择性酶促酯化拆分反应进行
了放大,放大 50 倍至克级,e.e.值仍能达到 100%。
参考文献:
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4 50 45 100 (下转第 1222 页)