Lim Yeeun, Breitbach Zachary S, Armstrong Daniel W, Berthod Alain
Department of Chemistry, University of Texas at Arlington, Planetarium Place, Arlington, TX 76019, USA.
Institut des Sciences Analytiques, CNRS, Université de Lyon, 5 rue de la Doua, 69100 Villeurbanne, France.
J Pharm Anal. 2016 Dec;6(6):345-355. doi: 10.1016/j.jpha.2016.07.003. Epub 2016 Jul 22.
It is a challenge to separate the enantiomers of native chiral amines prone to deleterious silanol interactions. A set of 39 underivatized chiral primary amines was screened for enantiomeric separation. Seven recently introduced commercial chiral columns were tested. They included six polysaccharide based chiral stationary phases (CSP) with bonded derivatives, ChiralPak® IA, IB, IC, ID, IE and IF columns and a cyclofructan derivatized CSP, Larihc® CF6-P column. Both the normal phase (NP) mode with heptane/alcohol mobile phases and the polar organic (PO) mode with acetonitrile/alcohol were evaluated. It was found that the cyclofructan based CSP demonstrated the highest success rate in separating primary amines in the PO mode with only one chiral amine not resolved. It is shown that, when screening the columns, there is no standard optimal condition; an excellent mobile phase composition for one column may be poorly suited to another one. Although butylamine was a good mobile phase additive for the polysaccharide columns in both PO and NP modes, it was detrimental to the enantio-recognition capability of the cyclofructan column. Triethylamine was the appropriate silanol screening agent for this latter column.
分离天然手性胺的对映体颇具挑战,因为其易产生有害的硅醇相互作用。对39种未衍生化的手性伯胺进行了对映体分离筛选。测试了七种最近推出的商用手性柱。它们包括六种带有键合衍生物的多糖基手性固定相(CSP),即ChiralPak® IA、IB、IC、ID、IE和IF柱,以及一种环糊精衍生的CSP,Larihc® CF6-P柱。评估了使用庚烷/醇流动相的正相(NP)模式和使用乙腈/醇的极性有机(PO)模式。结果发现,基于环糊精的CSP在PO模式下分离伯胺的成功率最高,只有一种手性胺未分离。结果表明,在筛选柱子时,没有标准的最佳条件;一种柱子的出色流动相组成可能并不适合另一种柱子。尽管丁胺在PO和NP模式下都是多糖柱的良好流动相添加剂,但它会损害环糊精柱的对映体识别能力。三乙胺是后一种柱子合适的硅醇筛选剂。