白地霉G38生物转化制备抗忧郁药(R)-fluoxetine

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％。

Microbial-chemical routes to R and S-denopamine a useful drug for congestive heart failure

Both enantiomers of denopamine were synthesized using microbial-chemical approach via bioreduction of 1-(acetoxyphenyl)ketone 4(R=CH2Cl) and 5(R=CO(2)Et) with fungus Geotrichum sp. G38.