手性药物前体R(-)-扁桃酸的生物不对称合成  

Asymmetric synthesis of chiral precursor R(-)-mandelic acid

作　　者：郭黛苹[1] 李忠琴[1] 杨凯[1] 杨元营[1] 许小平[1] 

机构地区：[1]福州大学化学化工学院,福建福州350002

出　　处：《中国医学工程》2006年第6期576-578,共3页China Medical Engineering

基　　金：福建省自然科学基金资助项目(C0410006)

摘　　要：目的研究生物不对称催化苯乙酮酸合成手性药物前体R(-)-扁桃酸。方法通过对该实验室保存的12株酵母菌进行初筛,获得对底物苯乙酮酸具有较高催化活性的菌株S.c.1,S.c.3和S.c.10。进一步对其进行紫外与微波诱变,得到R(-)-扁桃酸高产菌株S.c.10.2.8。结果在转化培养中,初始底物浓度为20mmol/L,pH6.6,温度34℃,R(-)-扁桃酸得率85%,对映体过量值e.e>99%。结论生物转化法在生产手性药物前体R(-)-扁桃酸中前景广泛。[Objective] To study the synthesis of chiral precursor R（-）-mandelic acid obtained by asymmetric bioreduction of phenylglyoxylic acid. [Methods] Saccharomyces cerevisiae strains S.c.1, S.c.3 and S.c.10 were selected as original strains for further screening higher production of chiral precursor R（-）-mandelic acid. The mutant strain S.c.10.2.8 possessing effective transformaing ability and almost absolute enantioselectivity was obtained with the methods of ultraviolet and microwave mutagenesis. [Results] Under the conditions of initial substrate concentration 20mmol/L, pH6.6, temperature 34℃. The yield and the enantiomeric excesses of R（-）-mandelic acid were 85% and 99% respectively. [Conclusion] Biotransformation is a potential alternative method producing chiral precursor. R（-）-mandelic acid.

关 键 词：R(-)-扁桃酸 手性 生物转化 

分 类 号：O621.34[理学—有机化学]