Biginelli Reaction Of Aliphatic Aldehydes Catalyzed By Alpha-Chymotrypsin: One-Pot Biocatalytic Synthesis Of Dihydropyrimidinones

A green and highly efficient procedure was developed for the one-pot, three-component synthesis of 3,4-dihydropyrimidin-2-(1H)-ones by the condensation of aliphatic aldehydes, beta-keto esters, and urea. alpha-Chymotrypsin from porcine pancreas showed excellent catalytic activity in the reaction. The influences of solvents, temperature, and water content were investigated. The desired products were obtained in 85-96% yields. The methodology generates high yields with a wide range of substrates.