Late Transition Metal Catalysts for Organic Synthesis

有机合成用后过渡金属催化剂

• 批准号: 8755679
• 负责人: STEPHEN L BUCHWALD
• 金额: $ 55.46万
• 依托单位: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-09-01 至 2018-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8755679
• 关键词: Academia; Adverse effects; Alcohols; Alkanesulfonates; Alkenes; Amination; Amines; Applications Grants; Biomedical Research; Carbon; Catalysis; Chemistry; Complex; Copper; Coupling; Development; Drug Industry; Evolution; Goals; Hand; Imines; Improve Access; Industry; Investigation; Kinetics; Lead; Ligands; Medicine; Metals; Methodology; Methods; Nitrogen; Organic Chemistry; Organic Synthesis; Oxygen; Pharmaceutical Chemistry; Pharmacologic Substance; Phenols; Preparation; Process; Property; Resolution; Science; Techniques; Temperature; Transition Elements; Vertebral column; Work; analog; aryl halide; base; catalyst; cost; drug discovery; functional group; improved; novel; pi bond; public health relevance; sensor; small molecule; user-friendly

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.

描述（由申请人提供）：功能化分子的可用性在有机化学和药物化学领域以及制药和相关行业中具有极其重要的意义。不仅要使化合物易于获得，而且要使其易于和可预测地进行修饰以改变其性质和/或消除副作用的方法具有重大意义。本资助申请中提出的化学涉及发明或强化技术，以获取含有碱性氮中心的分子作为关键结构特征。我们之前在这一领域的工作已经被纳入合成有机化学家的日常曲目，并极大地影响了有机合成领域，特别是在制药工业的药物发现方面。此外，我们还建议从极其简单的（烯烃）前体合成各种胺的对映体纯（单手）形式。基本上所有现代小分子药物现在都必须以单手形式销售，这一壮举的成功完成可能会增加药物制剂的成本。本文还介绍了氮杂环化合物制备的新方法。在许多方面，这类化合物构成了制药工业的支柱。我们还建议对包括在内的所有化学成分进行机理研究。此外，从这项工作中获得的信息将有助于了解正在发展的进程的机制，以便提高我们正在发展的方法的效率。总的来说，成功实现本资助申请中提出的化学将对化学家和辅助领域的化学家开发新的重要医学，传感器或生物学相关的能力产生重大影响