Han W W, Yakatan G J, Maness D D
J Pharm Sci. 1977 Apr;66(4):573-7. doi: 10.1002/jps.2600660429.
The hydrolysis kinetics of oxazepam and diazepam leading to a benzophenone product and a glycine derivative were quantified from pH 1 to 11. For oxazepam, two intermediates were isolated and identified, indicating a parallel consecutive reaction mechanism. The hydrolysis occurred uncatalyzed and demonstrated acid-base catalysis for both reaction steps. One intermediate was observed by TLC for diazepam hydrolysis. This intermediate, resulting from breakage of the azomethine linkage, was different than the major intermediate isolated for oxazepam hydrolytic degradation (amide hydrolysis preferred). Stability parameters involving rate constant-temperature dependence are reported.
在pH值1至11的范围内，对导致二苯甲酮产物和甘氨酸衍生物生成的奥沙西泮和地西泮的水解动力学进行了定量分析。对于奥沙西泮，分离并鉴定出两种中间体，表明其反应机制为平行连续反应。水解反应未受催化，但在两个反应步骤中均表现出酸碱催化作用。通过薄层色谱法观察到地西泮水解过程中的一种中间体。该中间体由偶氮甲碱键断裂产生，与奥沙西泮水解降解过程中分离出的主要中间体（酰胺水解优先）不同。报告了涉及速率常数与温度依赖性的稳定性参数。
