Water-soluble Derivatives of Vitamin D2. I. Preparation and Properties of Vitamin D2-phosphoric Acid Ester.

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Abstract
An improved method for the phosphorylation of vitamin D2 with phosphorus oxychloride in ether and pyridine has been described. Two reaction products, compounds I and II, have been isolated and studied. Compound I, which was the main product, had no antirachitic effect in vivo. The infrared spectrum of this substance indicated that the vitamin had been modified during phosphorylation. In in vivo studies, compound II showed antirachitic effects comparable to those of unphosphorylated vitamin D2. When compound II was administered to rachitic rats, the time interval between dosing and the appearance of a demonstrable effect on calcium absorption and skeletal deposition was as long as the interval for the unphosphorylated vitamin. Hydrolysis to phosphoric acid and vitamin D2 may occur prior to the exertion of antirachitic activity of compound II in vivo.

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