α-糜蛋白酶催化合成3, 4-二氢嘧啶-2(1H)-酮

Synthesis of 3, 4-dihydropyrimidin-2(1H)-ones catalyzed by α-chymotrypsin

摘要:

以α-糜蛋白酶为生物催化剂，通过芳香醛、尿素和乙酰乙酸乙酯之间的Biginelli反应合成3,4-二氢嘧啶-2(1H)-酮类化合物，并对反应条件进行了优化。得到的最佳反应条件为：反应介质为乙醇，芳香醛、乙酰乙酸乙酯和尿素的物质的量比为1:1.5:1，α-糜蛋白酶用量为20 mg，反应温度为50℃，反应时间为96 h。在该条件下，合成3,4-二氢嘧啶-2(1H)-酮衍生物，产率为55~63%。该法具有反应条件温和、操作简单、底物适用范围较广等优点。

Abstract:

3,4-Dihydropyrimidin-2(1H)-ones were synthesized via α-chymotrypsin-catalyzed Biginelli reaction between aromatic aldehyde, urea and ethyl acetoacetate. Through optimization, the optimal reaction conditions were obtained as follows: the reaction medium was ethanol, the molar ratio of aromatic aldehyde to ethyl acetoacetate and urea was 1:1.5:1, the amount of α-chymotrypsin was 20 mg, the reaction temperature was 60℃ and the reaction time was 96 h. Under this optimum reaction conditions, a series of 3,4-dihydropyrimidin-2(1H)-ones derivatives having a yield of 55% to 63% were obtained. The method has the advantages of mild reaction conditions, simple operation and broad application range of the substrates.