High Selective Synthesis of 11α-hydroxycanrenone by Biotransformation

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.