目的 在有机相中利用酶促反应合成能被去唾液酸糖蛋白受体(ASGPR)特异性识别的配体胆固醇-半乳糖苷分子,对其合成工艺进行优化.方法 采用质谱和核磁碳谱鉴别产物结构;单因素和正交设计法优化酶促合成条件.结果 酶促最佳条件为底物胆固醇癸二酸乙烯酯(CH-VS)与乳糖醇(LA)物质的量之比4:1,脂肪酶Novozym 435 25 mg,反应32 h,产率高达92%.结论 该方法高效、反应条件可行、产物专一.

Objective To synthesize asialoglycoprotein receptor (ASGPR) ligand cholesterol-vinyl sebacate-lactitol (CH-VS-LA) by using enzymatic reaction in organic phase and to optimize its synthesis process. Methods MS and ¹³C-NMR were used to identify the structure of product, enzymatic synthesis conditions were optimized via single-factor test and orthogonal experimental design. Results The enzymatic optimum conditions were as following: the molar ratio of cholesterol-vinyl sebacate (CH-VS) and lactitol (LA) was 4:1, the amount of lipase Novozym 435 was 25 mg, reactional time was 32 h, and productive rate was 92%. Conclusion The method is highly effecient, the reaction conditions are reasonable, and the process produces no by-product.

教育部高等学校博士学科点专项科研基金(20134425110010)