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NEW METHODS FOR THE SYNTHESIS OF BIOACTIVE MOLECULES

合成生物活性分子的新方法

基本信息

批准号：
6627170
负责人：
NICOS A PETASIS
金额：
$ 26.32万
依托单位：
UNIVERSITY OF SOUTHERN CALIFORNIA
依托单位国家：
美国
项目类别：
财政年份：
1992
资助国家：
美国
起止时间：
1992-07-01 至 2004-06-30
项目状态：
已结题

项目摘要

This research program explores new reactions of organoborn compounds and their application in short and practical preparations of bioactive substances. In addition to the studying the scope and limitations of the key reactions, this program also explores a number of synthetic strategies where the new chemistry is combined with the other powerful chemical transformation. In this manner it becomes possible to synthesize diverse multifunctional molecules rapidly and efficiently. The specific aims of this project are: 1. New chemical reactions: a main focus of this project is the further development of the Bronco Acid Mannish reaction, a novel one-step three-component process that gives new amine or amino acid derivatives By reacting an amine with and organobornic acid or borate with certain carnal compounds. Studies are focussed on mechanistic and sterochemical aspects, and the use of functionalist organoborn derivatives. 2. New synthetic strategies: This project pursues a number of selected strategies that demonstrate the utility of the new reactions for the synthesis of various bioactive molecules. These studies combine the new chemistry with several other powerful and versatile chemical processes, including other multi component reactions, acylations, metal catalyzed coupling, olefin metathesis, and various cycloadditions. 3. Synthesis of bioactive molecules: Another goal of this synthesis of selected types of bioactive molecules that are easily accessible with the new chemistry. The targeted molecules include: pepitdomimetics, a variety of substituted heterocycles, polyol amines, aminosugars, and various molecular scaffolds as well as oligomeric systems for probing protein interactions. Overall, the chemistry in this program has a number of advantages, such as the introduction of multiple functional groups and the control of steroechemistry. It also faculties the synthesis of numerous new bioactive molecules for further studies. Therefore, this program makes new advances in organic, medicinal and combinatorial chemistry, and enhances the role of organic synthesis in biomedical research.

本研究计划探索有机含硼化合物的新反应及其在短而实用的生物活性物质制备中的应用。除了研究关键反应的范围和局限性外，这个项目还探索了一些合成策略，其中新的化学与其他强大的化学转化相结合。通过这种方式，可以快速高效地合成各种多功能分子。本项目的具体目标是：1.新的化学反应：本项目的一个主要重点是进一步发展Bronco酸Mannish反应，这是一种新的一步三组分工艺，通过将胺与有机硼酸或硼酸盐与某些肉质化合物反应得到新的胺或氨基酸衍生物。研究集中在机械和立体化学方面，以及官能化有机硼衍生物的使用。2.新的合成策略：这个项目追求一些精选的策略，这些策略证明了新反应在合成各种生物活性分子方面的实用性。这些研究将新的化学与其他几个强大和多功能的化学过程相结合，包括其他多组分反应、酰化、金属催化偶联、烯烃歧化和各种环加成反应。3.生物活性分子的合成：这种合成的另一个目标是合成选定类型的生物活性分子，这些分子很容易用新的化学方法获得。目标分子包括：儿茶素、各种取代杂环、多元醇胺、氨基糖和各种分子支架以及用于探测蛋白质相互作用的低聚体系。总体而言，该计划中的化学具有许多优势，如引入多个官能团和控制立体化学。它还使许多新的生物活性分子的合成成为可能，以供进一步研究。因此，该计划在有机、药物和组合化学方面取得了新的进展，并增强了有机合成在生物医学研究中的作用。