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。
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 .
出处
《微生物学通报》
CAS
CSCD
北大核心
2007年第2期221-223,共3页
Microbiology China
关键词
坎利酮
11α-羟坎利酮
微生物转化
Canrenone, 11α-hydroxycanrenone, Microbial transformation