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。方法通过对本实验室保存的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-1,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 higher production of chiral precursor R( - ) -mandelic acid. The mutant strain S. c. 10. 2. 8 possessing effective transforming ability and almost absolute enantioselectivity was obtained using ultraviolet and microwave mutagenesis. RESULTS Under the conditions of initial substrate concentration 20 mmol · L^-1, pH 6. 6, temperature 34 ℃, the yield and the enantiomeric excesses of R( - ) -mandelic acid were 85% and 99% respectively. CONCLUSION Biotransformaton is a potential alternative method to produce chiral precursor R( - )-mandelic acid.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2007年第7期550-553,共4页
Chinese Pharmaceutical Journal
基金
福建省自然科学基金资助项目(C0410006)