非水相酶促合成萘普生油酸甘油酯前药

摘要

在非相有机试剂异辛烷中通过固定化脂肪酶Novozym435催化萘普生甲酯与三油酸甘油酯反应，通过薄层层析色谱与高效液相色谱对反应液进行分析，并考察了底物摩尔比、反应时间、反应温度、酶添加量、溶剂添加量对转化率的影响。结果表明，当三油酸甘油酯与萘普生甲酯摩尔比3.85，反应时间144h，反应温度50℃，酶添加量150mg，溶剂添加量5mL时，转化率最高达到65.91%。%The synthesis of a new type prodrug for naproxen-oleylglycerol through the lipase-catalyzed trans-esterification of naproxen and triolein was studied. The reaction was indentified by TLC and HPLC and the influen-tial factors of substrate molar ratio,reaction time,reaction temperature,enzyme amount and isooctane amount were systematically investigated.Results indicated that in the reaction system the optimal conditions as follows n(SN):n(TO)=3.85,reaction time 144h reaction temperature 50℃,enzyme amount 150mg and 5mL Isooctane added.Under the optimal conditions the maximum yield was obtained as high as 65.91%.