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Recognition of Acyl Donors by Lipase CAL-B in the Acylation of 6-Azauridine

机译:脂肪酶CAL-B在6-氮杂尿苷酰化中对酰基供体的识别

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CAL-B-catalyzed synthesis of different 5'-O-monoester derivatives of 6-azauridine via a one-step highly regioselective enzymatic acylation route was successfully performed for the first time. The effects of some crucial factors on the enzymatic undec-10-enoylation of 6-azauridine were examined. The optimal reaction medium,molar ratio of 6-azauridine to vinyl undec-10-enoate and reaction temperature were found to be anhydrous acetone,1:3 and 50°C,under which the reaction rate,the substrate conversion and the regioselectivity were 22.3 mMlh,99.0% and 99.0%,respectively. In addition,the enzyme recognition of acyl donors was investigated. The results showed that the enzyme activity varied widely with different acyl donors owing to the specific structure of the lipase active site and the acyl donors. 5'-O-Monoesters of 6-azauridine were achieved exclusively with all the acyl donors tested.
机译:首次成功地通过一步高区域选择性酶促酰化途径成功进行了CAL-B催化的6-氮杂嘧啶5'-O-单酯衍生物的合成。研究了一些关键因素对6-氮杂尿苷酶促十一碳烯基化的影响。最佳反应介质为:无水丙酮,1:3、50°C,6-氮杂嘧啶与十一碳烯酸乙烯酯的摩尔比和反应温度为22.3,反应速率,底物转化率和区域选择性为22.3。 mMlh分别为99.0%和99.0%。另外,研究了酰基供体的酶识别。结果表明,由于脂肪酶活性位点和酰基供体的特定结构,不同酰基供体的酶活性变化很大。仅用所有测试的酰基供体获得6-氮杂嘧啶的5'-O-单酯。

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