Enantiomeric Scaffolds for Organic Synthesis

用于有机合成的对映体支架

• 批准号: 7392356
• 负责人: LANNY S LIEBESKIND
• 金额: $ 30.6万
• 依托单位: EMORY UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1989
• 资助国家: 美国
• 起止时间: 1989-12-01 至 2011-02-28
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7392356
• 关键词: Air; Biological; Chemicals; Chemistry; Communities; Complex; Condition; Development; Disease; Facility Construction Funding Category; Family; Future; Ligands; Medical; Metals; Methods; Molecular; Molecular Structure; Organic Synthesis; Pharmaceutical Chemistry; Pharmaceutical Preparations; Production; Public Health; Range; Research; Research Design; drug discovery; enantiomer; improved; novel; programs; rapid technique; scaffold; small molecule

DESCRIPTION (provided by applicant): This research program seeks to provide the medicinal chemistry and drug discovery communities with practical and effective methods for the rapid and enantiocontrolled construction of diverse, biologically relevant molecular motifs from conceptually simple, yet synthetically powerful "enantiomeric scaffolds". The easy production in quantity of single enantiomers of inexpensive, air-stable metal pi-complexes of unsaturated heterocyclic organic ligands provides "organometallic chirons" whose flexible and novel synthetic elaboration can generate, after demetalation, a highly varied range of biologically significant molecular structures in an enantiospecific fashion. This research, both in progress achieved to date and in the future research design and methods demonstrates that enantiomeric scaffolding using organometallic chirons is a valuable and versatile strategy for enantiocontrolled synthesis and for the exploration of chemical space. The development of new small molecule drugs for the treatment of disease, for the amelioration of debilitating medical conditions, and for improving the general state of health of the public relies to a significant extent on the synthetic power of chemistry. This research describes a general strategy to carry out the highly controlled synthesis of structurally divergent families molecules with demonstrated medical and biological applications.

描述（由申请人提供）：本研究计划旨在为药物化学和药物发现群落提供实用有效的方法，用于从概念上简单，合成具有合成功能的“对烯剂” caffolds的快速和对照控制构建不同的生物学相关的分子基序。不饱和的杂环有机配体的廉价，空气稳定的金属PI复合物的单一对映异构体的易于生产，可提供“有机金属奇兰”，其灵活而新颖的合成阐述可以在脱离后产生，在脱离后，在生物学上重要的分子结构在entiperspecepienty e Enantispecific senantipersion senantipersixific senantipersific senantiperific senantiperific senantiperific senantiperific senantiperific。这项研究是迄今为止实现的以及未来的研究设计和方法表明，使用有机金属chirons进行对映体脚手架是对映射合成和化学空间探索的宝贵而多才多艺的策略。开发用于治疗疾病的新小分子药物，减轻衰弱的医疗状况以及改善公众的总体健康状况，在很大程度上取决于化学的合成能力。这项研究介绍了一种一般策略，该策略是通过证明的医学和生物学应用进行高度控制的结构分歧家族分子的合成。