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在甾体激素化合物的C_(16)上加入甲基,则疗效增強副作用減失。 (1)新法引进16α-甲基合成16α-甲基-9α-氟-1-脫氢考的唑(dexamethasone)。作者发现一个简便的新法,将易于生成的16β-甲基变为16α-甲基,同时又生成17α-羟基如下所示。化合物Ⅱ—Ⅳ,都分别证明其结构。从Ⅳ经若干步合成化合物Ⅴ,此物能变为16α-甲基-9α-氟-1-脱氢考的唑是已知的事实。
In the steroid hormone compounds C_ (16) on the methyl, the efficacy of increased side effects loss. (1) The new method introduces 16α-methyl synthetic 16α-methyl-9α-fluoro-1-dehydroxybenzothiazole. The authors found a simple new method to change easily-formed 16β-methyl to 16α-methyl while producing 17α-hydroxyl as shown below. Compounds Ⅱ-Ⅳ, respectively, to prove its structure. It is known from the synthesis of compound V from IV by several steps that this can become a 16α-methyl-9α-fluoro-1-dehydroxybenzazole.