NMR SPECTROSCOPIC CHARACTERIZATION OF ADINAZOLAM MESYLATE - PH-DEPENDENT STRUCTURE CHANGE IN AQUEOUS-SOLUTION AND ACTIVE METHYLENE

被引：2

作者：

OGATA, M

TAHARA, T

NISHIMURA, T

机构：

[1] Analytical Research and Specifications Development, Tsukuba Research Laboratories, Upjohn Pharmaceuticals Limited, Tsukuba-Shi, Ibaraki, 300-42

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1995年 / 84卷 / 06期

关键词：

D O I：

10.1002/jps.2600840624

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The present study is to investigate structural changes of adinazolam mesylate in aqueous solution under various pH conditions by NMR spectroscopy. By plotting of the signal integration and chemical shifts of the side chain, pK(a) Values for imine hydrolysis and the side chain amine were determined. Conformational analysis of the side chain was performed with deuterium-induced isotope effects on chemical shifts, nuclear Overhauser effects, relaxation times, and energy calculations. Hydrogen/deuterium exchange due to an active methylene at the 4-position under basic conditions was revealed.

引用

页码：786 / 790

页数：5

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