在特定碱和通用碱存在下N-(羟甲基)邻苯二甲酰亚胺的水相降解。氮杂环N-羟甲基衍生物作为潜在前药的动力学评估。

Aqueous degradation of N-(hydroxymethyl)phthalimide in the presence of specific and general bases. Kinetic assessment of N-hydroxymethyl derivatives of nitrogen heterocycles as possible prodrugs.

作者信息

Khan M N

机构信息

Department of Chemistry, Bayero University, Kano, Nigeria.

出版信息

J Pharm Biomed Anal. 1989;7(6):685-91. doi: 10.1016/0731-7085(89)80112-8.

DOI:10.1016/0731-7085(89)80112-8

PMID:2490772

Abstract

The conversion of N-(hydroxymethyl)phthalimide (NHPH) to phthalimide could not be detected within 300 s at pH 9.0, whereas in 0.18 M NaOH complete conversion of NHPH to phthalimide was observed within 50 s. In the presence of 0.2-0.4 M 1,4-diazabicyclo[2.2.2]octane buffer solutions (pH 9.30-9.54), 40-60% conversion of NHPH to phthalimide occurred within 90-120 s. The initial concentration of NHPH affected the extent of conversion of NHPH to phthalimide.

摘要

在pH 9.0的条件下，300秒内未检测到N-（羟甲基）邻苯二甲酰亚胺（NHPH）转化为邻苯二甲酰亚胺，而在0.18 M氢氧化钠中，50秒内观察到NHPH完全转化为邻苯二甲酰亚胺。在0.2 - 0.4 M 1,4 - 二氮杂双环[2.2.2]辛烷缓冲溶液（pH 9.30 - 9.54）存在的情况下，90 - 120秒内NHPH有40 - 60%转化为邻苯二甲酰亚胺。NHPH的初始浓度影响NHPH向邻苯二甲酰亚胺的转化程度。