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）：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行业中具有极其重要的意义。不仅化合物应该易于获取，而且容易且可预测地修饰它们以改变其性质和/或消除副作用的方法也具有巨大的意义。本资助申请中提出的化学涉及发明或强化获取含有碱性氮中心作为关键结构特征的分子的技术。我们之前在该领域的工作已融入有机合成化学家的日常工作中，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，我们还提议从极其简单的（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独的形式出售，而这一壮举的成功实现可能会增加药剂的成本。还包括制备氮杂环的新方法。在许多方面，此类化合物构成了制药工业的支柱。我们还建议对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理解正在开发的过程的机制，以提高我们正在开发的方法的效率。总体而言，本次拨款申请中提出的化学的成功实现将对化学家和辅助领域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进步的化合物和材料。