探讨了连续流动反应器中动力学拆分1,1,1-三氟异丙胺(TFPA)的可行性,比较了3种脂肪酶的催化效果及其对连续流动与间歇搅拌反应的影响。结果表明,连续流动反应方式下,以Novozym 435为催化剂,65℃下在装载固定化脂肪酶的色谱柱内停留3 min,1,1,1-三氟异丙胺的转化率可达到50%,产物N-[(1R)-2,2,2-三氟-1-甲基乙基]-乙酰胺的对映体过量值(ee)高达99.5%,且连续反应50 h后酶的活性保持原有水平,表观米氏常数为4.8 mmol/L;而采用间歇搅拌方式、反应时间为8 h时,转化率仅为41.6%。

The feasibility of kinetic resolution of 1,1,1-trifluoro-isopropyl amine is explored in a continuous flow reactor.Catalytic effects of three kinds of common lipases are compared,and their effects on continuous flow and intermittent stirring reaction respectively are compared.Studies show that the conversion rate of 1,1,1-trifluoroisopropylamine can reach 50% and the enantiomeric excess value of product N-[(1R)-2,2,2-trifluoro-1-methyl-ethyl]-acetamide is as high as 99.5% when Novozym 435 is used as catalyst,the temperature is at 65℃,the retention time is 3 minutes and the reaction is performed under continuous flow mode.Furthermore,the activity of lipase remains it original level after 50 hours of continuous reaction,and apparent Michaelis constant is 4.8 mmol·L^-1.The conversion rate is only 41.6% after 8 hours of reaction and intermittent stirring mode is employed.