Enzymes, which provide more efficient and eco-friendly strategies for various functional molecules’ construction than traditional chemo-catalysts, were utilized for the synthesis of 4H-pyrimido[2,1-b] benzothiazole derivatives. Reported herein is a trypsin-catalysed three- component Biginelli reaction of aldehyde, β-ketoester and 2-amino benzothiazole in one pot, affording a streamlined pathway to diverse ring-fused pyrimidines. In addition to using commercially available aromatic aldehydes as substrates, acetaldehyde, the chemical liquid with rather low boiling point and difficult to handle above room temperature, is utilized to further extend the range of substrates. It was verified that most of the tested substrates exhibited satisfactory reactivity. In addition, several substrates indicated AIE (Aggregation-Induced Emission) property and have been investigated as potential biomarkers.

与传统的化学催化剂相比，酶为各种功能分子的构建提供了更有效和更环保的策略，被用于合成4H-嘧啶[2,1- b] 苯并噻唑衍生物。本文报道了一种胰蛋白酶催化的醛、β-酮酯和 2-氨基苯并噻唑在一个锅中的三组分 Biginelli 反应，提供了一条通向各种稠环嘧啶的流线型途径。除了使用市售的芳香醛作为底物外，乙醛这种沸点较低且在室温以上难以处理的化学液体也被用于进一步扩展底物的范围。经证实，大多数测试底物表现出令人满意的反应性。此外，几种底物表明了 AIE（聚集诱导发射）特性，并已被研究为潜在的生物标志物。