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中文摘要
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描述(由申请人提供):功能化分子的可用性在有机和药物化学领域以及制药和相关工业中具有极其重要的意义。不仅化合物应该是可获得的,而且容易和可预测地对它们进行修饰以改变它们的性质和/或消除副作用的方法也具有巨大的意义。在这项拨款申请中提出的化学涉及到发明或强调访问包含碱性氮中心作为关键结构特征的分子的技术。我们以前在这一领域的工作已经融入了合成有机化学家的日常工作,并对有机合成领域产生了巨大影响,特别是在制药行业的药物发现方面。此外,我们还建议以非常简单的(烯烃)前体为原料,以对映体纯(单手)形式合成多种胺。基本上,所有现代小分子药物现在都必须以单手形式销售,成功完成这一壮举可能会增加药物制剂的成本。还包括制备含氮杂环化合物的新方法。在许多方面,这类化合物构成了制药业的支柱。我们还建议对包括在内的所有化学物质进行机理研究。此外,从这项工作中获得的信息将有助于理解正在开发的过程的机制,以便提高我们正在开发的方法的效率。总的来说,这项资助申请中提出的化学的成功实现将对化学家和辅助领域的人员开发新的医学上重要的传感器或生物相关的能力产生重大影响。 将推动科学向前发展的化合物和材料。
英文摘要
DESCRIPTION (provided by applicant): The availability of functionalized molecules is of preeminent importance in the fields of organic and medicinal chemistry and to the pharmaceutical and related industries. Not only should compounds be accessible, but also the means to readily and predictably modify them to change their properties and/or eliminate side effects is of tremendous significance. The chemistry that is proposed in this grant application involves the invention or accentuation of techniques to access molecules that contain basic nitrogen centers as key structural features. Our prior work in this field has been incorporated into the everyday repertoire of synthetic organic chemists and has greatly impacted the field of organic synthesis, particularly in drug discovery in the pharmaceutical industry. In addition, we are proposing work on the synthesis in enantiomerically pure (single handed) form of a wide variety of amines from extremely simple (alkene) precursors. Essentially all modern small molecule medicines must now be sold in single-handed forms and the successful accomplishment of this feat can add to the cost of the medicinal agent. Also included are new methods for the preparation of nitrogen heterocycles. In many ways, compounds of this type form the backbone of the pharmaceutical industry. We also propose to carry out mechanistic studies on all of the chemistry included. Further, information gained from this work will help to understand the mechanism of the processes that are being developed in order to increase the efficiency of the methods that we are developing. Overall, the successful realization of the chemistry proposed in this grant application will have a major impact on the ability of chemists and those in auxiliary fields to develop new medicinally important, sensor or biologically relevant compounds and materials that will move science forward.
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Metal-Catalyzed Methods for Organic Synthesis
Metal-Catalyzed Methods for Organic Synthesis
Metal-Catalyzed Methods for Organic Synthesis
Metal-Catalyzed Methods for Organic Synthesis
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