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甾体激素往往因分子中在 C_6的α-位置加入一甲基而增强其疗效,例如6α-甲基可的松及6α-甲基可的唑(Ⅰ)均比其母体的功效大得多,黄体酮在 C_(17)上加入一乙酰氧基可使其疗效较为持久,若再在 C_6-α位置上加入甲基则不但疗效比母体大五、六十倍,并可内服,而黄体酮则只能注射,此物(Ⅺ)的已知合成方法中,似以 Babcock 等的方法较为简便。其法是用17α-羟基黄体酮(Ⅱ)为原料,即先作成 A 环上应有的不饱和酮簇,然后再加入6α-甲基,最后引入17α-乙酰氧基得Ⅺ。
Steroid hormones are often enhanced by the addition of a methyl group to the α-site of C_6 in the molecule. For example, both 6α-methyl cortisone and 6α-methyl-oxazolone (I) are much more potent than their parent counterparts , Progesterone in C_ (17) by adding acetoxy can be more lasting effect, if the C_6-α position in the addition of methyl is not only the efficacy of five or six times more than the mother, and can be taken orally, while the corpus luteum Ketones can only be injected, this (XI) of the known synthesis methods, like Babcock and other methods is more convenient. The method is to use 17α-hydroxy progesterone (Ⅱ) as a raw material, that is, a ring of unsaturated ketones should be formed first in the ring, and then add 6α-methyl, and finally introduce 17α-acetoxy to give XI.