YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
難水溶性医薬品の水溶性誘導体の合成 (第4報)
ステロイド燐酸エステル誘導体
森 芳夫
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ジャーナル フリー

1961 年 81 巻 12 号 p. 1674-1677

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Steroids can be made soluble in water by derivation to the salt of a secondary phosphate. Synthesis of a secondary phosphate including a steroid was attempted on hydrocortisone with phosphorylation agent of the ROPOCl2 type but the product obtained was a bis-hydrocortisone ester. With the reagent of (RO)2POCl type, esterification using this reagent with R as phenyl gave a tertiary phosphate which easily liberated one phenyl to form the phosphate of steroid and phenyl by treatment with potassium carbonate at room temperature. With this reagent where R is benzyl, the tertiary phosphate obtained by esterification also lost one benzyl group to form a secondary phosphate by treatment with sodium iodide or lithium chloride.

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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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