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近年来在寻找治疗效果更好的雌激素药物的研究中,发现某些11-羟基取代的衍生物有显著提高活性的效果。同时又发现一系列11β-羟基取代的雄甾衍生物是一类高选择性强效纯糖皮质激素新型抗炎药物,其糖皮质甾抗炎活性可比地塞米松强2～3倍,而盐皮质甾副作用仅为地塞米松的数十分之一。然目前对雄甾和雌甾底物还没有很好的微生物11-上羟的方法,用化学方法上羟也是至今尚未很好解决的课题。 我们参考文献方法,以副肾皮质激素氢化泼尼松1为原料。经边链降解可方便地得至11β-羟基雄甾
In recent years in the search for estrogen drugs with better therapeutic effects, certain 11-hydroxy-substituted derivatives have been found to have significantly improved activity. At the same time, it was also found that a series of 11β-hydroxy substituted androsta derivatives are a kind of highly selective and potent pure glucocorticoid new anti-inflammatory drugs with anti-inflammatory activity of glucocorticoids 2-3 times stronger than that of dexamethasone, while salts Corticosteroid side effects are only one-tenth of dexamethasone. However, at present, there is not a very good method for the microorganism 11-hydroxylation of the androsteroids and estrogens, and the chemical method is still a problem that has not been solved yet. We reference method to the adrenocorticotropic hormone prednisolone 1 as raw material. The 11β-hydroxyandrostol is readily available by side chain degradation