4 MONTH BIOMED GRANT LETTER WAS SENT TO D DEERFIELD

4 个月的 Biomed 授权信已发送给 D DEERFIELD

• 批准号: 6220991
• 负责人: PETER A KOLLMAN
• 金额: $ 2.78万
• 依托单位: MELLON PITTS CORPORATION (MPC CORP)
• 依托单位国家: 美国
• 财政年份: 1999
• 资助国家: 美国
• 起止时间: 1999-08-01 至 2000-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6220991
• 关键词: bioengineering /biomedical engineering; biological products; biomedical resource; computers; drug /agent

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.

一种常见的非甾体抗炎药布洛芬以外消旋混合物的形式销售。 它是 然而，旋光异构体更具商业价值 特别是对于制药行业。 过去几年内 多年来，研究人员已经能够通过以下方法分离对映体： 使用 L-赖氨酸作为分离剂的传统结晶技术 代理人。 这个过程虽然成功，但很耗时，因为 取决于晶体的形成。 超临界流体的使用 提供了一种快速且廉价解决问题的潜在方法。 我们 开发了一种适用于超临界碳的拆分剂 二氧化碳介质。 通过初步的分子建模研究，使用 阿林格 MM3 力场的增强形式，该特工出现 对布洛芬的对映体有足够的选择性 理论基础。 我们已经综合并表征了我们的 拆分剂，是一种氟化的L-赖氨酸衍生物。 我们的 对映体布洛芬的尝试与理论展望 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。