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应用固定化直链淀粉手性固定相开发新型单胺氧化酶 B 抑制剂。

Application of an immobilised amylose-based chiral stationary phase to the development of new monoamine oxidase B inhibitors.

机构信息

Istituto Superiore di Sanità, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy.

出版信息

Talanta. 2010 Jun 30;82(1):426-31. doi: 10.1016/j.talanta.2010.04.039. Epub 2010 Apr 24.

DOI:10.1016/j.talanta.2010.04.039
PMID:20685489
Abstract

A direct HPLC enantioseparation of three new chiral oxadiazoline derivatives endowed with potential MAO-B inhibitory activity was accomplished on the immobilised Chiralpak IA chiral stationary phase. Multi-mg amounts of enantiomers with high enantiomeric purity (ee> or =98%) were rapidly collected using pure dichloromethane as eluent. The absolute configuration and chiroptical properties of the enantiomers isolated at semipreparative scale were exhaustively determined.

摘要

采用手性固定相 Chiralpak IA,通过直接高效液相色谱对 3 种新型手性恶二唑啉衍生物进行对映体拆分,实现了潜在的 MAO-B 抑制活性。使用纯二氯甲烷作为洗脱剂,快速收集到毫克级对映体,且对映体纯度高(ee>或=98%)。在半制备规模下对分离得到的对映体的绝对构型和旋光性质进行了详尽的确定。

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引用本文的文献

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