论文部分内容阅读
分别测定了2-萘基丙酸类药物萘普生R-、S-对映体在有机溶剂中的酶促酯化反应初速度，并研究了反应温度、酰基受体和有机溶剂等反应条件对脂肪酶的反应活性和对映选择性的影响。在一定范围内，酶反应活性随温度升高而增加，温度过高易使酶失活；酶选择性则随温度升高而下降；反应温度以35～40℃为佳。在疏水性强的溶剂中，酶反应活性较大；酶的选择性则以异辛烷、苯、甲苯等为溶剂时较好。合适的混合溶剂系统能使酶表现出比在单一溶剂中更好的活性和选择性；这与外消旋萘普生的实际酶促拆分结果是一致的。
The initial rates of enzymatic esterification of 2-naphthylpropionic acid naproxen R- and S-enantiomers in organic solvents were determined respectively. The reaction conditions such as reaction temperature, acyl acceptor and organic solvents Effect on lipase reactivity and enantioselectivity. In a certain range, the enzyme activity increases with increasing temperature, the enzyme is inactivated when the temperature is too high, and the enzyme selectivity decreases with the increase of temperature. The reaction temperature is preferably 35-40 ℃. In the hydrophobic solvent, the enzyme activity is greater; the selectivity of the enzyme is isooctane, benzene, toluene, etc. as solvent is better. A suitable mixed solvent system enables the enzyme to show better activity and selectivity than in a single solvent; this is consistent with the actual enzymatic resolution of racemic naproxen.