11α-羟坎利酮的高特异性生物转化合成

High Selective Synthesis of 11α-hydroxycanrenone by Biotransformation

摘要:

坎利酮是合成心血管疾病药物Eplerenone的重要中间体，其关键的C₁₁α-羟化反应可以由微生物转化完成。本实验室保藏的根霉（Rhizopus sp.SIPI-0602）可特异性地将坎利酮转化为化合物SIPI-11。通过测定与分析SIPI-11的UV、MS和NMR图谱数据，确定化合物SIPI-11为11α-羟坎利酮。摇瓶转化工艺研究表明，底物投料浓度不高于6g/L时，11α-羟坎利酮的转化率可达到90％以上。

Abstract:

Canrenone is an important intermediate for the synthesis of eplerenone，a cardiovascular drug.C₁₁α-hydroxylation of canrenone is the key reaction，which can be done by microbial transformation.Rhizopus sp.SIPI-0602，kept in our lab，could high selectively transform canrenone to a compound named SIPI-11.By determining and analyzing the MS，UV，NMR etc.spectra of compound SIPI-11，its chemical structure was elucidated to be 11α-hydroxycanrenone.The study on flask transformation technology showed that the transformation ratio exceeded 90% when the substrate concentration was not more than 6g/L.