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手性药物前体R(-)-扁桃酸的生物不对称合成 被引量:3

Study on Asymmetric Synthesis of Chiral Precursor R(-)-mandelic Acid
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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)
关键词 R(-)-扁桃酸 手性 生物转化 R ( - ) -mandelic acid chrlal biotransformation
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