Optimization of enzymatic synthesis of asialoglycoprotein receptor ligand cholesterol-vinyl sebacate-lactitol / 中草药

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.