4 MONTH BIOMED GRANT LETTER WAS SENT TO D DEERFIELD

一种常见的非甾体抗炎药，布洛芬，作为外消旋混合物上市。它是 然而，光学活性异构体更具商业价值。 尤其是对制药业。在过去的几年里 多年来，研究人员已经能够通过以下方法分离对映体 以L-赖氨酸为拆分的传统结晶技术 探员。这一过程虽然成功，但很耗时，因为它 取决于晶体的形成。超临界流体的使用 为快速、廉价地解决问题提供了一种潜在的手段。我们 已经开发出一种适用于超临界碳的拆分剂 二氧化物介质。通过初步的分子建模研究 作为Allinger MM3力场的一种扩展形式，该代理出现 对布洛芬对映体具有足够的选择性 理论基础。我们已经合成并表征了我们的 拆分剂，它是一种含氟的L-赖氨酸衍生物。我们的 布洛芬对映体的尝试和理论期望 超临界二氧化碳的分离将与 手性氨基酸系统在非传统介质中的有效性。

A common NSAID, ibuprofen, is marketed as a racemic mixture. It's optically active isomer however, is more commercially valuable particularly to the pharmaceutical industry. Within the past few years investigators have been able to separate the enantiomers by traditional crystallization techniques using L-lysine as a resolving agent. This process, though successful, is time consuming because it is dependent upon crystal formation. The use of supercritical fluids affords a potential means to quick and inexpensive resolution. We have developed a resolving agent suitable for a supercrititcal carbon dioxide medium. Through preliminary molecular modeling studies using a augmented form of Allinger's MM3 force field, this agent appears sufficiently selective for the enantiomers of ibuprofen on a theoretical basis. We have synthesized and characterized our resolving agent, which is a fluorinated L-lysine derivative. Our attempts and theoretical expectations of enantiomeri ibuprofen separations in supercritical carbon dioxide will be related to the effectiveness of chiral amino acid systems in non-traditional media.