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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。
Objective To synthesize Bestatin derivatives stereoselectively. Methods Four racemic mixtures with the same structural formula were isolated using a common silica gel column in combination with L-amino acid methyl ester hydrochloride as a chiral derivatization reagent. Results Twelve of Bestatin derivatives were successfully synthesized and isolated. The inhibitory activity in vitro showed that compounds such as 12a, 13a and 15a inhibited the activity of aminopeptidase N (APN). Conclusion The experimental method can synthesize the bestatin derivative stereoselectively, but the absolute configuration of the compound needs to be determined.