Efficient biocatalytic strategy for one-pot Biginelli reaction via enhanced specific effects of microwave in a circulating reactor

Abstract

A one-pot efficient biocatalytic strategy for the synthesis of 3,4-dihydropyrimidin-2-(1H)-ones was developed in a circulating microwave reactor selecting α-chymotrypsin as the promiscuous biocatalyst. In the circulating reaction system, the combination of microwave heating and external cooling could avoid the denaturation and inactivation of enzyme, and greatly improved the radiation power of microwave, thus improving the specific effects of microwave. During the reaction process, the microwave radiation power was automatically adjusted by adjusting the speed of the reaction mixture circulation. When the microwave power was maintained at 110 W, the best results could be obtained with the highest yield of 96% at 55 °C in 50 min, and the reaction had a wide range of substrates. But no obvious product was detected in a tank microwave reactor at 55 °C for 100 min, under this condition, the microwave power was maintained at about 3 W. As a contrast, the reaction only obtained 63% yield in 55 °C oil bath for 96 h.

Keywords: Biginelli reaction; Biocatalysis; Circulating microwave reactor; Non-natural activity; Specific effects of microwave.