医薬品の分解とその安定化(第14報)アミノアルキルエステルの構造と安定性についてその6

概要

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Diphenylacetic acid esters of 2-diethylaminoethanol (I), 3-diethylaminopropanol (II), 4-diethylaminobutanol (III), 5-diethylaminopentanol (IV) and 6-diethylamino hexanol (V) were synthesized and the effect of the number of methylenes in the aminoalkyl esters on the rate of hydrolysis in an aqueous buffered solution was examined. Increase in the number of methylenes in the alkyl group of the aminoalkylesters decreased the hydrolysis rate constants in the alkaline side but not in the acidic side. In these series of compounds, there was a correlation between the observed pKa value and the logarithm of the hydrolysis rate constants (k_<OH>). The esters containing a large number of methylenes were very stable and the formation of micelle was observed in aqueous solution.
公益社団法人日本薬学会の論文
1976-01-25