A novel and efficient strategy for the synthesis of phosphoramidon and its β anomer has been developed by manipulating the anomerization of α-l-rhamnose triacetate upon phosphitylation. The experimental results suggest that proton transfer, bond rotation, and N atom are the key factors for the anomerization. The determined K_i and K_d values establish that phosphoramidon prepared by this method possesses excellent biological activity, and indicate that the contacts of rhamnose moiety with the enzyme have limited contribution to the binding.

中文翻译：

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磷酰胺及其β端基异构体的合成和酶学评估：α-1鼠李糖三乙酸酯在磷酸化作用下的异构化

一种用于磷酸阿米酮及其β端基异构体的合成新颖的和有效的策略已经通过操纵的α-端基异构开发升在亚磷酸化鼠李糖三乙酸酯。实验结果表明，质子转移，键的旋转，和N原子都为端基异构化的关键因素。所确定的ķ_我和ķ _d值建立通过该方法制备的磷酸阿米酮具有优良的生物活性，并表明鼠李糖部分的与酶接触必须结合有限的贡献。