一种新的异氰酸酯类手性衍生化试剂用于药物对映体高效液相色谱拆分性能的研究

A NEW CHIRAL DERIVATIZING REAGENT FOR THE RESOLUTION OF AMINE AND ALCOHOL DRUG ENANTIOMERS BY HPLC

在已报道的四十多种手性衍生化试剂中,异氰酸酯是应用研究最活跃的一类。目前,这类试剂只有(R)-(-)或(S)-(+)-naphthylethyl isocyanate(NEIC)和(R)-(+)或(S)-(-)-phenylethyl isocyanate(PEIC)两种。它们均由相应的手性伯胺化合物,经光气或氯甲基硅烷作用得到的。但光气是毒性极大的气体。

A new chiral derivatizing reagent (s) -α - methoxybenzyl isocyanate (MIB) was prepared from (s) - (+) - mandelic acid with a practical method, and its ability of liquid chromatographic rasolution for drug enantiomers by pre-column chiral derivatization was evaluated with racemic amphetamine and mexiletine as well as phenylpropanol. The operation is simple and rapid. Separation is good for the amine isomers, but poor for alcohols and extensive work remains to be done. The solution of derivatization was directly injected into the chromatograph. Conventional silica gel column was used with light petroleum as the mobile phase.