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目的:采用酶催化法在非水相介质中合成半乳糖配体。方法:通过IR,质谱,核磁共振(1H-NMR,1C-NMR)对产物结构进行表征;以底物转化率为指标,采用单因素试验考察酶种类、反应介质、酶加入量、底物摩尔比、反应温度等对配体合成的影响。结果:通过表征分析显示经酶的催化反应,半乳糖C1’位的羟基发生了酯化反应,所得产物为目标产物。优选的反应条件为反应介质四氢呋喃(THF)-二甲基亚砜(DMSO)(3∶1),Novozym 435固定化脂肪酶为催化剂,酶加入量600 U.mL-1,半乳糖-硬脂酸乙烯酯的摩尔比1∶4,于55℃反应8 h,半乳糖的转化率达>0%。结论:酶促催化法可用于合成肝靶向脂质体配体。
OBJECTIVE: To synthesize galactose ligands in non-aqueous medium by enzyme catalysis. Methods: The structure of the product was characterized by IR, MS, 1H-NMR and 1 C-NMR. The substrate conversion was taken as the index. The enzyme type, reaction medium, enzyme dosage, Ratio, the reaction temperature on the ligand synthesis. Results: Through the characterization and analysis, the esterification reaction was carried out on the hydroxyl group at the C1 ’position of galactose through the catalytic reaction of the enzyme. The obtained product was the target product. The optimal reaction conditions were reaction medium of tetrahydrofuran (THF) -dimethylsulfoxide (DMSO) (3: 1), Novozym 435 immobilized lipase as catalyst, enzyme dosage 600 U.mL-1, galactose- Acid vinyl ester molar ratio of 1: 4, at 55 ℃ for 8 h, the conversion rate of galactose> 0%. Conclusion: Enzymatic catalysis can be used to synthesize liver-targeted liposome ligands.