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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)
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