Enantiomeric Scaffolds for Organic Synthesis

描述（由申请人提供）：本研究项目旨在为药物化学和药物发现界提供实用有效的方法，用于从概念简单但合成功能强大的“对映体支架”中快速和对映控制地构建各种生物相关的分子基序。廉价的、空气稳定的不饱和杂环有机配体的金属双配合物的单对映体的容易生产提供了“有机金属chirons”，其灵活和新颖的合成精加工可以在脱金属后以对映特异性的方式产生高度多样化的生物重要分子结构。这项研究，无论是迄今为止取得的进展，还是在未来的研究设计和方法中，都表明使用有机金属chirons的对映体支架是对映体控制合成和探索化学空间的一种有价值和通用的策略。用于治疗疾病、改善衰弱的医疗状况和改善公众健康状况的新型小分子药物的开发，在很大程度上依赖于化学的合成能力。本研究描述了一种总体策略，以进行高度控制的合成结构不同的家庭分子与演示医学和生物学的应用。

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.