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中文摘要：
目的立体选择性地合成Bestatin衍生物。方法利用普通的硅胶加压柱联合L-氨基酸甲酯盐酸盐作为手性衍生化试剂将具有同一结构式的4个外消旋混合物进行了分离。结果成功地合成并分离了Bestatin衍生物12个，体外抑酶活性表明12a、13a、15a等化合物有较高的抑制氨肽酶N（APN）的活性。结论该实验的方法能立体选择性地合成Bestatin的衍生物，但化合物的绝对构型还有待确定。
英文摘要：
Aim The derivatives of Bestatin were synthesized stereoselectively. Methods Combined normal silica pressure column with L-aa-OCH3· HCI as chiral pool, four racemic mixtures were synthesized and separated. Results 12 Bestatin＇s derivatives were synthesized and separated successfully, and activity assay in vitro showed that compounds 12a,13a and 15a had high inhibitory activities against APN. Conclusion The method we used could stereoselectively synthesize Bestatin＇s derivatives. The determination of the absolute configurations of our target compounds is under way.
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