文章摘要
谢宗波.α-糜蛋白酶催化合成3, 4-二氢嘧啶-2(1H)-酮[J].精细化工,2019,36(8):
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
投稿时间:2018-10-12  修订日期:2019-02-21
DOI:
中文关键词: Biginelli反应  α-糜蛋白酶  3, 4-二氢嘧啶-2(1H)-酮  生物催化  芳香醛
英文关键词: Biginelli reaction  α-chymotrypsin  3, 4-dihydropyrimidin-2(1H)-ones  biocatalysis  aromatic aldehyde
基金项目:
作者单位E-mail
谢宗波 东华理工大学 zbxie@ecit.cn 
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中文摘要:
      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。
英文摘要:
      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.
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