Chiral separations using fluorous triphasic chemistry

使用氟三相化学进行手性分离

基本信息

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
项目类别：
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

项目摘要

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）：Fluorof Technologies，Inc。将开发和商业化其专有的易流性三重技术，以分离手性化合物。由于监管需求增加和产品线扩展，因此单一对映异构体药物目前在市场上占主导地位，并将在将来继续这样做。这些单个对映异构体化合物以具有成本效益的方式合成可能具有挑战性。流畅的三重技术有可能成为分离对映异构体的经济过程，几乎不需要高危的资本投资。长期的目的是提供一种具有催化，选择性和连续的技术，该技术为其他分离方法提供了一种具有成本效益的替代方案。还设想了超出简单分离和多反应序列的技术的应用。 I阶段授予的目标是证明该过程可以在荧光组件中催化，并可以应用于单一对映异构体药物的合成。具体目的是： 1）使用催化易流的载体证明三联体分离。 2）在不预先标记的情况下表现出手性分离。 3）证明可以将荧光三重反应用于单个对映异构体药物的形式合成。