Lingeman H, Haan H B, Hulshoff A
J Chromatogr. 1984 Dec 12;336(2):241-8. doi: 10.1016/s0378-4347(00)85147-6.
A rapid and selective derivatization procedure is described for the pre-column labelling of carboxylic acids with a nitrogen-containing label. The carboxylic acid function is activated with 2-bromo-1-methylpyridinium iodide and the activated carboxylic acid function reacts with a primary or a secondary amine to yield an amide. With flurbiprofen as the test compound and dipropylamine as a label the acid was completely converted to the corresponding amide. The method was tested for several aliphatic, aromatic and for phenylacetic or phenylpropionic carboxylic acid derivatives, and was found to result in the complete derivatization of these compounds with a few exceptions only. The derivatization procedure is potentially useful for drug monitoring purposes, as is shown with the analysis of valproic acid and flurbiprofen in plasma.
描述了一种快速且选择性的衍生化方法，用于用含氮标记物对羧酸进行柱前标记。羧酸官能团用2-溴-1-甲基碘化吡啶活化，活化后的羧酸官能团与伯胺或仲胺反应生成酰胺。以氟比洛芬为测试化合物，二丙胺为标记物，该酸完全转化为相应的酰胺。该方法针对几种脂肪族、芳香族以及苯乙酸或苯丙酸羧酸衍生物进行了测试，结果发现除了少数例外，这些化合物都能完全衍生化。如在血浆中丙戊酸和氟比洛芬的分析所示，该衍生化方法在药物监测方面具有潜在用途。
