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白地霉G38生物转化制备抗忧郁药(R)-fluoxetine
ISOLATION OF A STRAIN OF HIGH ACTIVITY OF DICARBONYL COMPOUND REDUCTION——GEOTRICHUM sp. G38 AND USED IN PREPARATION OF (R)-FLUOXETINE
【摘要】 从200株菌中筛选出具有双酮化合物还原活力较高的菌株7株,其中以白地霉(Geotrickum, sp. )G38活力最高,而且有较好的区域选择性和立体选择性。白地霉G38能对β-羰基苯丙酸乙酯进行不对称还原,生成(R)-β-羟基苯丙酸乙酯,用于制备抗忧郁药(R)-fluoxetine。用二甲基硅橡胶包埋白地霉菌体取代游离菌体进行生物转化,可以提高反应的立体选择性,对映体过量值从49％提高到81％。
【Abstract】 Seven strains of microorganisms which have activity of dicarbonyl compound reduction were isolated, in which Geotrichum sp. G38 showed the highest activity and good regioselectivity and stereoselectivity. Using Geotrichum sp. G38, ethyl benzoylacetate was reduced to (R)-ethyl 3-Phenyl-3-hydroxy propionate which was the intermediate in preparing (R)-fluoxetine. The ee value was improved from 49% to 81% when silicone-immobilized cells was used instead of free cells in biotransformation.
【关键词】 生物转化；
白地霉；
G38；
β-羰基苯丙酸乙酯；
(R)-fluoxetine；
【Key words】 Biotransformation； Geotrichum sp. G38； Ethyl benzoylacetate； (R)- fluoxetine；
【Key words】 Biotransformation； Geotrichum sp. G38； Ethyl benzoylacetate； (R)- fluoxetine；
【基金】 中国科学院“八·五”重点应用项目
- 【文献出处】 微生物学报 ,Acta Microbiologica Sinica , 编辑部邮箱 ,1995年05期
- 【分类号】TQ464
- 【被引频次】16
- 【下载频次】107