alpha-Chymotrypsin-catalyzed direct C (Sp(3))-H functionalization reactions for synthesis of azaarene derivatives in water

摘要

alpha-Chymotrypsin from the bovine pancreas has been shown for the first time to display catalytic nonnatural catalytic ability toward the C (sp(3))-H functionalization reaction of 2-methylquinoline and aromatic aldehydes in water. alpha-Chymotrypsin exhibited favorable catalytic activity with good adaptability to different substrates. The activity of the enzyme could be improved by adjusting the solvent, temperature, molar ratio of substrates, and protein loading. The products were obtained in moderate to excellent yields (51%-93%) in 24 samples. This process afforded a potential biocatalytic approach as an alternative to chemical synthesis for azaarene derivatives.