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

作　　者：姜佳雯 孙立瑞 李海艳[1] 辛嘉英[1,2] 夏春谷[2] 

机构地区：[1]哈尔滨商业大学食品科学与工程省重点试验室,黑龙江哈尔滨150076 [2]中国科学院兰州化学物理研究所羰基合成和选择氧化国家重点试验室,甘肃兰州730000

出　　处：《化学工程师》2016年第2期16-19,8,共5页Chemical Engineer

基　　金：黑龙江省应用技术研究与开发计划项目(No.GC13C111)2-芳基丙酸类药物的酶法手性拆分

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%.

关 键 词：萘普生油酸甘油酯 脂肪酶 非水相 

分 类 号：O643.32[理学—物理化学]