拟低共熔体系中脂肪酶水解拆分萘普生酯

In this paper, methyl 2-(6-methoxy-2naphthyl)propionate(naproxen)was asymmetrically hydrolyzed by candida rugosa lipase in pseudo-eutectic and organic solvent systems. The result showed that S -(+)-naproxen with enantiomeric excess more than 95% could be obtained with commercially available candida rugosa lipase in both systems. In organic solvent system, 24.1% reaction conversion of naproxen methylester could be obtained after 96 hours, while in pseudo-eutectic systems, the conversion was 40.1% after 72 h. Furthermore,only one fifth organic solvent volume was used in pseudo-eutectic systems.Compared to organic solvent systems, the effects of lipase concentration, substrate and water concentration, and several different kinds of adjuncts on reaction conversion were studied in pseudo-eutectic system. Also,under the optimium pseudo-eutectic enzymatic reaction conditions, the reaction conversion was 45.8%.

化学-酶法合成RGD三肽

采用化学法和酶法相结合的合成策略,合成具有高生物活性肽RGD。先采用DCC合成GD二肽(HCl·Gly Asp(oBzl)2),然后利用胰蛋白酶(trypsin)催化合成RGD三肽(Z Arg GlyAsp(oBzl)2)。实验结果表明,其中GD二肽在反应10h,两底物G与D的摩尔比为1 5∶1时,得率为77 7%;RGD三肽在微水-1,4-丁二醇反应体系中得率为41 9%。

化学法合成RGD三肽的研究

采用二环己基碳二亚胺法(DCC)合成了二肽Gly Asp(OBzl) 2 ,然后利用混合酸酐法得到全保护RGD三肽:Boc Arg(NO2 ) Gly Asp(OBzl) 2 三肽;最后在Pd/C的催化加氢下,将保护基一起脱掉而得到RGD三肽的粗品。具体研究了合成二肽及三肽的主要影响因素及其优化条件。在优化条件下,获得三肽的结晶干品,总得率为5 7 2 %。