Chiral separations using fluorous triphasic chemistry

使用氟三相化学进行手性分离

• 批准号: 6832916
• 负责人: Marvin S Yu
• 金额: $ 11.96万
• 依托单位: FLUOROUS TECHNOLOGIES, INC.
• 依托单位国家: 美国
• 财政年份: 2004
• 资助国家: 美国
• 起止时间: 2004-08-01 至 2006-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6832916
• 关键词: chemical synthesis; combinatorial chemistry; drug design /synthesis /production; enzyme activity; fluorine; physical separation; reagent /indicator; stereochemistry; stereoisomer; technology /technique development

DESCRIPTION (provided by applicant): Fluorous Technologies, Inc. will develop and commercialize its proprietary fluorous triphasic technology for the separation of chiral compounds. Due to increased regulatory demands and product line extensions, single enantiomer drugs currently dominate the marketplace and will continue to do so in the future. The synthesis of these single enantiomer compounds in a cost effective manner can be challenging. Fluorous triphasic technology has the potential to be an economical process for the separation of enantiomers requiring little at-risk capital investment. The long term aim is to provide a technology which is catalytic, selective, and continuous that provides a cost effective superior alternative to other separation methods. The application of the technology beyond simple separations and into multi-reaction sequences is also envisioned. The goals of the Phase I grant are to demonstrate that the process can be catalytic in the fluorous component and can be applied to the synthesis of a single enantiomer drug. The specific aims are: 1) To demonstrate a fluorous triphasic separation using a catalytic fluorous carrier. 2) To demonstrate a chiral separation in a fluorous triphasic reaction without pre-tagging. 3) To demonstrate that a fluorous triphasic reaction can be used in the formal synthesis of a single enantiomer pharmaceutical.

描述(申请人提供)：氟技术公司将开发其用于手性化合物分离的专有氟三相技术并将其商业化。由于监管要求的增加和产品线的延长，单一对映体药物目前主导着市场，并将在未来继续这样做。以经济有效的方式合成这些单一的对映体化合物可能是具有挑战性的。氟三相技术有可能成为一种经济的分离对映体的过程，只需要很少的风险资本投资。长期的目标是提供一种催化的、选择性的和连续的技术，提供一种比其他分离方法更具成本效益的优越选择。还展望了该技术在简单分离之外的多反应序列中的应用。第一阶段赠款的目标是证明该过程在氟成分中可以是催化的，并且可以应用于单一对映体药物的合成。 具体目标是： 1)展示使用催化氟载体的氟三相分离。 2)在氟三相反应中进行手性拆分，无需预标记物。 3)证明了氟三相反应可用于单一对映体药物的合成。