非水相酶促合成萘普生油酸甘油酯前药

Synthesis of naproxen-oleylglycerol prodrug by nonaqueousphase enzyme- catalyzed reactions

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5m L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- esterifieation 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,reaetion temperature,enzyme amount and isooetane amount were systematieally investigated.Results indicated that in the reaetion system the optimal conditions as follows n（SN）：n （TO）=3.85,reaetion 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%.