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（由申请人提供）：Fluorous Technologies，Inc.将开发和商业化其专有的氟三相技术，用于手性化合物的分离。由于监管需求的增加和产品线的延伸，单一对映体药物目前主导市场，并将在未来继续如此。以成本有效的方式合成这些单一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方法，用于分离对映体，需要很少的风险资本投资。长期目标是提供一种催化、选择性和连续的技术，该技术提供了比其它分离方法更经济的上级替代方法。该技术的应用超出了简单的分离，并进入多反应序列也被设想。第一阶段赠款的目标是证明该过程可以在氟组分中起催化作用，并可应用于单一对映体药物的合成。 具体目标是： 1)目的：演示使用催化氟载体的氟三相分离。 2)证明在无预标记的氟三相反应中的手性分离。 3)证明氟三相反应可用于单一对映体药物的形式合成。