Miller Larry, Grill Charles, Yan Tony, Dapremont Olivier, Huthmann Elke, Juza Markus
Pharmacia, 4901 Searle Parkway, Skokie, IL, USA.
J Chromatogr A. 2003 Jul 18;1006(1-2):267-80. doi: 10.1016/s0021-9673(03)00782-9.
The preparative chromatographic resolution of racemates has become over the past few years a standard approach for the generation of enantiomers in pharmaceutical research and development. This paper will discuss the chromatographic resolution of a racemic pharmaceutical intermediate. Initial analytical method development to determine the best preparative conditions will be presented. Batch resolution of kg quantities of racemate followed by the simulated moving bed resolution of tens and hundreds of kg of racemate will also be discussed. Finally the different approaches used for the separation will be compared.
在过去几年中,外消旋体的制备色谱拆分已成为药物研发中制备对映体的标准方法。本文将讨论一种外消旋药物中间体的色谱拆分。将介绍用于确定最佳制备条件的初始分析方法开发。还将讨论千克量外消旋体的间歇拆分,以及数十千克和数百千克外消旋体的模拟移动床拆分。最后,将比较用于分离的不同方法。