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2報)
四級アンモニウム塩型誘導体
森 芳夫中川 俊夫
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ジャーナル フリー

1961 年 81 巻 7 号 p. 972-975

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Pharmaceutics sparingly soluble in water but possessing a hydroxyl group were led into quaternary ammonium-type derivatives to give water solubility. The compounds were first led to bromoacetate by application of bromoacetyl bromide in pyridine and addition of tertiary amine to its product gave the quaternary ammonium salts. Pharmaceutics used were hydrocortisone (Ia), prednisolone (Ib), and dexamethasone (Ic). The amines used were trimethylamine, triethylamine, N4-methyl-morpholine, pyridine, and triethanolamine for (Ia) and triethylamine for (Ib) and (Ic), using acetone as the solvent for addition reaction, becuase the use of alcohol as a solvent resulted in alcoholysis and the objective could not be obtained. The quaternary ammonium-type derivatives (III) synthesized formed crystals with the exception of pyridine adduct and their pharmacological activity was about equal to that of sodium hydrogensuccinate derivatives.

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