Late Transition Metal Catalysts for Organic Synthesis

有机合成用后过渡金属催化剂

基本信息

批准号：
9111922
负责人：
STEPHEN L BUCHWALD
金额：
$ 56.96万
依托单位：
MASSACHUSETTS INSTITUTE OF TECHNOLOGY
依托单位国家：
美国
项目类别：
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

项目摘要

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.

描述（由申请人提供）：在有机和药物化学领域以及药物和相关行业的官能化分子的可用性至关重要。不仅应该可以访问化合物，而且还可以轻松修改它们以改变其特性和/或消除副作用的方法具有巨大的意义。本赠款应用中提出的化学涉及的化学涉及发明或强调技术以获取包含基本氮中心作为关键结构特征的分子。我们在该领域的先前工作已纳入了合成有机化学家的日常曲目中，并极大地影响了有机合成领域，尤其是在制药行业的药物发现中。此外，我们还提出了从极其简单（烷烃）前体的多种胺的对映体纯（单手）形式的合成的工作。本质上，所有现代小分子药物现在都必须以单手形式出售，并且成功完成此壮举可以增加药物剂的成本。还包括用于制备氮杂环的新方法。在许多方面，这种类型的化合物构成了制药行业的骨干。我们还建议对包括所有化学的机械研究进行机械研究。此外，从这项工作中获得的信息将有助于了解正在开发的过程的机制，以提高我们开发的方法的效率。总体而言，在本赠款应用中提出的化学反应的成功实现将对化学家和辅助领域的能力产生重大影响将推进科学的化合物和材料。