LATE TRANSITION METAL CATALYSTS FOR ORGANIC SYNTHESIS

用于有机合成的后过渡金属催化剂

• 批准号: 6788016
• 负责人: STEPHEN L BUCHWALD
• 金额: $ 54.62万
• 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: 1998-07-01 至 2006-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6788016
• 关键词: amidation /deamidation; catalyst; chemical synthesis; combinatorial chemistry; copper; cyclization; cycloalkene; drug discovery /isolation; heavy metals; indoles; microcalorimetry; organometallic compounds; palladium

DESCRIPTION (provided by applicant): The aims of this work are to develop new methods for organic synthesis and to examine applications of this methodology to the efficient preparation of medicinally interesting compounds. In particular methods to effect carbon-nitrogen and carbon-oxygen bond formation are proposed. The development of new synthetic methods is of central importance to the development of organic synthesis in particular and organic chemistry in general. The availability of general and predictable means by which to assemble large numbers of small molecules in both a specific as well as a combinatorial fashion is key to the uncovering of new lead structures in drug discovery. Moreover, the ability to quickly generate a diverse set of analogs of the initial lead compounds is essential for the rapid arrival at compounds with improved pharmacological profiles. Included in this work is the development of techniques that can lead to the ready availability of a wide collection of heterocyclic compounds. These compounds are the building blocks of medicinal chemistry and the pharmaceutical industry. The described methodology could have an immediate impact on the efficient access to a variety of important molecules, be they lead compounds in drug discovery or analogs of the initial leads that possess a better pharmacological profile.

描述（由申请人提供）：这项工作的目的是开发有机合成的新方法，并研究这种方法在有效制备医学上有趣的化合物中的应用。特别地，提出了实现碳-氮键和碳-氧键形成的方法。新合成方法的发展对有机合成和有机化学的发展具有重要意义。一般和可预测的手段，通过它来组装大量的小分子在一个特定的以及组合的方式是关键的发现新的先导结构的药物发现。此外，快速产生初始先导化合物的不同类似物组的能力对于快速获得具有改善的药理学特性的化合物是必不可少的。 包括在这项工作是技术的发展，可以导致广泛的杂环化合物的收集现成可用。这些化合物是药物化学和制药工业的基石。所描述的方法可以对有效获得各种重要分子产生直接影响，无论是药物发现中的先导化合物还是具有更好药理学特征的初始先导化合物的类似物。