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副肾皮质激素的分子中加入16α-羟基不但可以增加功效,并且可以消除钠储留的副作用。例如1-去氢-9α氟-16α-羟基-16α,17α-缩丙酮可的唑,不仅无钠的储留作用,而且抗炎功效大为增加。加入16α-羟基的化学方法甚多,但都不如生物羟基化的方法直接,例如用9α-氟可的唑为原料,用微生物Streptomyces roseochromogenus作用一步卽得加入16α-羟基之物,得率50％。我们企图用此种微生物在化合物s醋酸酯(I)的16位上加入α-羟基,借以合成所述的一类化合物。
Addition of 16? -hydroxy to the molecules of the adrenocortical hormone not only increases efficacy but also eliminates the side effects of sodium retention. For example, 1-dehydro-9α-fluoro-16α-hydroxy-16α, 17α-acetonide may not only have no sodium retention, but also greatly increase the anti-inflammatory effect. There are many chemical methods for adding 16α-hydroxyl groups, but none of them are as direct as bio-hydroxylation methods. For example, using 9α-fluorozoxazole as raw material, adding 16α-hydroxyl group with Streptomyces roseochromogenus in one step, the yield is 50% . We attempted to use this microorganism to add a-hydroxy group to the 16-position of Compound Acetate (I) to synthesize a class of compounds.