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采用短刺小克银汉霉菌 (CunninghamellablakesleanaAS 3.15 3)对普萘洛尔进行了代谢转化研究。液相色谱 多级质谱和核磁分析结果证明 ,转化液中主要含有 5 羟基普萘洛尔转化产物 ;考察了单羟化物形成的影响因素 ,发现在pH 6 .5、底物浓度 0 .2 5 %和转化反应持续 48h等条件下 ,5 羟基普萘洛尔的产率可达 76 % ,为活性药物代谢产物的合成开辟了一条新途径
Propranolol was metabolically transformed using Cunninghamella lakesleana AS 3.15 3. Liquid chromatography mass spectrometry and nuclear magnetic resonance analysis proved that the conversion solution mainly contains 5-hydroxypropyl-phenazine conversion products; investigated the formation of mono-hydroxylation factors and found that at pH 6.5, the substrate concentration of 0.55 % And conversion reaction for 48h and other conditions, the yield of 5-hydroxy-propranolol up to 76%, the synthesis of the active drug metabolites has opened up a new way