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The Development of New Stereoselective Organocatalytic Processes

新型立体选择性有机催化工艺的发展

基本信息

批准号：
8299496
负责人：
Jon Antilla
金额：
$ 25.43万
依托单位：
UNIVERSITY OF SOUTH FLORIDA
依托单位国家：
美国
项目类别：
财政年份：
2008
资助国家：
美国
起止时间：
2008-09-01 至 2013-07-31
项目状态：
已结题

项目摘要

DESCRIPTION (provided by applicant): Significant portions of important molecules involved in the biochemistry of life have "handedness," i.e. they are primarily found in one nonsuperimposible mirror image form. Additionally, the majority of drugs and drug candidates also have handedness (chirality) and all stereoisomers of these compounds are normally synthesized and evaluated for biological activity. Due to the chirality of nature, the mirror image forms of drug candidates can have vastly differing biological effects. One approach to the synthesis of chiral molecules that is growing steadily in usage is the application of versatile, stereoselective catalytic methodology in key steps where stereocontrol is required. Organocatalysis, the use of small organic (non-metal based) molecules as catalysts is an attractive alternative to traditional metal-based catalysis. This approach has found a number of recent successes and the continued evaluation of organocatalytic-based chemistry is clearly a worthwhile endeavor. Since 2004 the use of chiral phosphoric acid-based organocatalysis has been shown to provide for excellent stereoselectivity in a growing number of reactions. Our efforts have been involved in the development of new methodology where chiral phosphoric acids can be applied stereoselectively. The specific aims of this proposal are divided into the design, analysis, and refinement of a number of new reactions whereby chiral phosphoric acids can be efficient, stereoselective catalysts. The potential health-related utility of the newly created chiral products are also described in each new reaction study. PUBLIC HEALTH RELEVANCE: The chemistry described in this proposal addresses a fundamental, important aspect of modern synthesis -- the control of three-dimensional (3-D) chemical structure. The vast majority of the "molecules of life" and most pharmaceutical drugs have specific 3-D structure that must be controlled for efficient, low cost synthesis. Therefore methods that allow for this control are very important for public health.

描述（由申请人提供）：生命生物化学中涉及的重要分子的重要部分具有“手性”，即它们主要以一种不可重叠的镜像形式存在。此外，大多数药物和候选药物也具有手性（手性），这些化合物的所有立体异构体通常被合成并评估其生物活性。由于天然的手性，候选药物的镜像形式可能具有截然不同的生物效应。合成手性分子的一种稳步增长的方法是在需要立体控制的关键步骤中应用多功能立体选择催化方法。有机催化，使用小的有机（非金属基）分子作为催化剂是传统金属基催化的一个有吸引力的替代品。这种方法最近取得了一些成功，对基于有机催化的化学的持续评估显然是一项值得努力的工作。自2004年以来，手性磷酸基有机催化已被证明在越来越多的反应中具有优异的立体选择性。我们的努力已经参与开发新的方法，手性磷酸可以应用立体选择性。本提案的具体目的分为设计、分析和改进一些新的反应，手性磷酸可以成为有效的立体选择性催化剂。在每个新的反应研究中还描述了新创建的手性产物的潜在健康相关效用。公共卫生相关性：本提案中描述的化学解决了现代合成的一个基本而重要的方面——三维（3-D）化学结构的控制。绝大多数“生命分子”和大多数药物都具有特定的3-D结构，必须对其进行控制，才能高效、低成本地合成。因此，允许这种控制的方法对公共卫生非常重要。