Department of Complex Prescription of Traditional Chinese Medicine, China Pharmaceutical University, Long Mian Road 639, Nanjing 211198, PR China.
Bioorg Med Chem Lett. 2012 May 1;22(9):3100-3. doi: 10.1016/j.bmcl.2012.03.066. Epub 2012 Mar 21.
Lipase-catalyzed acylation of Guanfu alcohol-amine (GFAA) with vinyl acetate (VA) was performed in non-aqueous system for the preparation of Guanfu base G (GFG), a plant-originated alkaloid with significant antiarrhythmic activity. Among the eight lipases from different origins, Novozym 435 was found to be the best biocatalyst. The most suitable molecular sieve amount, substrate concentration, molar ratio of VA to GFAA, enzyme amount and reaction temperature were proved to be 40 mg/mL, 6 μmol/mL, 10:1, 2mg/mL and 50 °C, respectively. A maximum GFG yield of 37.4% was achieved under the selected conditions with methanol served as the optimal reaction medium. The structure of the acetylated product was elucidated by (1)H NMR and (13)C NMR analysis.
脂肪酶催化的 Guanfu 醇胺（GFAA）与醋酸乙烯酯（VA）的酰化反应在非水体系中进行，用于制备具有显著抗心律失常活性的植物来源生物碱 Guanfu 碱 G（GFG）。在来自不同来源的八种脂肪酶中，发现 Novozym 435 是最好的生物催化剂。证明最适宜的分子筛用量、底物浓度、VA 与 GFAA 的摩尔比、酶用量和反应温度分别为 40mg/mL、6μmol/mL、10:1、2mg/mL 和 50°C，甲醇为最佳反应介质时，乙酰化产物的最大收率为 37.4%。通过（1）H NMR 和（13）C NMR 分析阐明了乙酰化产物的结构。
