蔡祖恽, 高智强, 彭渤, 余新娣. 6α-甲基-17α-羟基-黄体酮和6α-甲基-17α-羟基-11去氧-皮质酮-21-乙酸酯的微生物羟化J. 药学学报, 1981, 16(5): 342-348.
引用本文: 蔡祖恽, 高智强, 彭渤, 余新娣. 6α-甲基-17α-羟基-黄体酮和6α-甲基-17α-羟基-11去氧-皮质酮-21-乙酸酯的微生物羟化J. 药学学报, 1981, 16(5): 342-348.
Cai Zuyun, Gao Zhiqiang, Peng Bo , Yu Xindi, . MICROBIOLOGICAL HYDROXYLATION OF 6α-METHYL-17α-HYDROXY PROGESTERONE AND 6α-METHYL-17α-HYDROXY-11-DEOXY-CORTICOSTERONE-21-ACETATEJ. Acta Pharmaceutica Sinica, 1981, 16(5): 342-348.
Citation: Cai Zuyun, Gao Zhiqiang, Peng Bo , Yu Xindi, . MICROBIOLOGICAL HYDROXYLATION OF 6α-METHYL-17α-HYDROXY PROGESTERONE AND 6α-METHYL-17α-HYDROXY-11-DEOXY-CORTICOSTERONE-21-ACETATEJ. Acta Pharmaceutica Sinica, 1981, 16(5): 342-348.

6α-甲基-17α-羟基-黄体酮和6α-甲基-17α-羟基-11去氧-皮质酮-21-乙酸酯的微生物羟化

MICROBIOLOGICAL HYDROXYLATION OF 6α-METHYL-17α-HYDROXY PROGESTERONE AND 6α-METHYL-17α-HYDROXY-11-DEOXY-CORTICOSTERONE-21-ACETATE

  • 摘要: 6α-甲基-11-去氧-17α-羟基-皮质酮-21-乙酸酯(Ⅱ)经短刺克宁汉霉微生物转化得6β-羟基化合物(Ⅵa)及6β,11β-羟基化合物(Ⅶa)。6α-甲基-17α-羟基-黄体酮(Ⅰ)经短刺克宁汉霉菌转化亦得6β-羟基化合物(Ⅵb)及6β,11β-羟基化合物(Ⅶb)。化合物(Ⅱ)如用梨头霉转化则得11α-羟化物(Ⅲ)。Ⅶa、Ⅶb、Ⅷa、Ⅷb及Ⅺb的结构是通过核磁共振谱和质谱证明的。

     

    Abstract: 6α-Methyl-11-deoxy-17α-hydroxy-corticosterone 21-acetate (Ⅱ) was transformed to compd Ⅵa and the new compd Ⅶa by Cunninghamella blakesleeana.Ⅵa was dehydrated to compd Ⅸa by p-toluensulfonic acid and transformed into a new compd Ⅷa by p-toluensulfonic acid in methanol Oxidizing compd Ⅶa with CrO3, compd Ⅺa was obtained. Similarily 6α-methyl-17α-hydroxy progesterone was transformed into compd Ⅵb and a new compd Ⅶb. Ⅵb also was dehydrated to compd Ⅸb and methylated in p-toluenesulfonic acid-methanol to a new compd Ⅷb. Using Absidia orchidis instead of Cunninghamella blakesleeana, compd Ⅱ was transformed to 11α-hydroxy compd Ⅲ.The structures of new compds Ⅶa, Ⅶb, Ⅶa, Ⅶb and Ⅺb were determined by spectroscopic evidences and chemical correlations.

     

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