微生物转化法合成7α,15α-二羟基雄烯醇酮  被引量:10

Synthesis of 7a,15a-Dihydroxyandrostenolone by Microbial Transformation

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作  者:尚珂[1] 胡海峰[1] 朱宝泉[1] 

机构地区:[1]上海医药工业研究院,上海200040

出  处:《中国医学生物技术应用》2004年第2期30-34,共5页The Chinese Academic Medical Magazine of Organisms

摘  要:7α,15α-二羟基雄烯醇酮1是合成口服避孕药Yasmin活性成分屈螺酮的重要中间体,应用亚麻刺盘孢(Colletotrichum lini AS 3.4486)的羟化酶系统对去氢表雄酮底物进行生物转化,合成了7α,15α-二羟基雄烯醇酮,转化率60~70%。转化机理研究发现,亚麻刺盘孢将底物的7位羟基化合成7α-羟基雄烯醇酮,再将其15位羟基化形成双羟基的产物。亚麻刺盘孢菌能够特异性、有序地完成对去氢表雄酮的两步羟化反应,与文献报道的结论一致,间接转化方法和转化机理属于首次报道。7α, 15α-dihydroxyandrostenolone is an important intermediate for synthesizing the drospirenone active ingredient of an oral contraceptive, Yasmin. It was obtained by bio-transforming androstenolone using Col-letotrichum lini AS 3.4486 in a yield of 60-70%. The study on the bio-transformation mechanism found that androstenolone was first transformed into 7α-hydroxy androstenolone, which then underwent 15β-hydrolation to produce the final product. This result suggested that C. lini AS 3.4486 can carry out two steps of hydroxylation reactions of androstenolone in a selective and sequential manner.

关 键 词:亚麻刺盘孢菌 雄烯醇酮 微生物转化 

分 类 号:R91[医药卫生—药学]

 

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