Enantiomeric Scaffolds for Organic Synthesis

描述（由申请人提供）：该研究计划旨在为药物化学和药物发现社区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”快速和对映体控制构建多样化的生物相关分子基序。不饱和杂环有机配体的廉价、空气稳定的金属π-络合物的单一对映体的大量容易生产提供了“有机金属手性子”，其灵活和新颖的合成加工可以在脱金属后以对映体特异性方式产生高度变化范围的生物学上重要的分子结构。这项研究，无论是在迄今为止取得的进展，并在未来的研究设计和方法表明，对映体支架使用有机金属手性是一个有价值的和通用的战略对映体控制的合成和化学空间的探索。用于治疗疾病、用于改善衰弱的医学状况以及用于改善公众的总体健康状况的新的小分子药物的开发在很大程度上依赖于化学的合成能力。本研究描述了一个一般策略，进行高度控制的合成结构不同的家庭分子与证明的医学和生物学应用。

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.