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在流动条件下使用两种市售丙炔酸酯对硫醇进行衍生化。

Derivatization of thiols under flow conditions using two commercially available propiolate esters.

机构信息

Laboratory of Analytical Chemistry, Department of Chemistry, Aristotelian University, GR-54124, Thessaloniki, Greece.

出版信息

J Pharm Biomed Anal. 2010 Nov 2;53(3):790-4. doi: 10.1016/j.jpba.2010.06.002. Epub 2010 Jun 8.

DOI:10.1016/j.jpba.2010.06.002
PMID:20580509
Abstract

In the present study we report new data on the reaction of three representative thiols--captopril (CAP), cysteine (CYS) and N-acetylcysteine (NAC)--with two commercially available propiolate esters--methyl-propiolate (MP) and butyl-propiolate (BP)--under flow conditions. The reactions were investigated on-line using sequential injection analysis (SI) and the formed derivatives were monitored spectrophotometrically at 285 nm. The effect of critical parameters of the reaction such as the pH, the temperature and the amount concentration of the reagents were studied in detail including stopped-flow (SF) experiments. Both reagents were found to be suitable for the automated derivatization of thiols, although MP offered faster kinetics compared to BP. The applicability of the procedures was demonstrated by the development of SI methods for the dissolution studies of CAP tablets with satisfactory results.

摘要

在本研究中,我们报告了三种代表性巯基化合物——卡托普利(CAP)、半胱氨酸(CYS)和 N-乙酰半胱氨酸(NAC)——与两种市售丙烯酸盐酯——甲基丙烯酸盐(MP)和丁基丙烯酸盐(BP)在流动条件下反应的新数据。该反应采用顺序注射分析(SI)在线进行研究,并在 285nm 处通过分光光度法监测形成的衍生物。详细研究了反应的关键参数,如 pH 值、温度和试剂的浓度,包括停流(SF)实验。结果表明,两种试剂都适合巯基的自动衍生化,尽管 MP 比 BP 具有更快的动力学。通过开发用于 CAP 片剂溶解研究的 SI 方法,证明了这些方法的适用性,结果令人满意。

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