α-糜蛋白酶催化合成β-脲基巴豆酸酯

α-Chymotrypsin-catalyzed Synthesis of β-Uramino Crotonic Ester

β-脲基巴豆酸酯是合成6-甲基嘧啶二酮衍生物及3,4-二氢嘧啶二酮衍生物的重要中间体,在生物制药中有着广泛的应用.由于酶具有绿色、安全、高效的催化特性,采用α-糜蛋白酶为生物催化剂,以N,N-二甲基甲酰胺为反应介质,37℃条件下,通过1,3-二羰基化合物和脲的缩合反应,合成了一系列β-脲基巴豆酸酯类化合物.

β-Uramino crotonic esters are important intermediate for the synthesis of 6-methylpyrimidinedione derivatives and 3,4-dihydropyrimidinedione derivatives,and they have a wide range of applications in biopharmaceuticals. Enzymes have green,safe and highly efficient catalytic properties,so a series of β-uramino crotonic esters was synthesized via the α-chymotrypsin-catalyzed condensation reaction between 1,3-dicarbonyl compounds and ureas at37 ℃ and in DMF medium.