11α-羟坎利酮的高特异性生物转化合成  

High Selective Synthesis of 11α-hydroxycanrenone by Biotransformation

作　　者：陶荣盛[1] 胡海峰[1] 李晓敦[1] 朱宝泉[1] 

机构地区：[1]上海医药工业研究院生物制药部,上海200040

出　　处：《微生物学通报》2007年第2期221-223,共3页Microbiology China

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 .

关 键 词：坎利酮 11α-羟坎利酮 微生物转化 

分 类 号：R914[医药卫生—药物化学]