Cascade C-N, C-O and C-S Bond Formation: Copper and Palladium Catalysed Synthesis of Heterocycle Arrays

本提案中的化学涉及一系列基于C-N， C-O， C-S和C-C偶联反应组合的级联过程的开发，由铜和钯基催化剂介导，以提供各种功能化的杂环产物。杂环核心的显著变化以及取代基的性质和位置将有可能采用本质上单一的策略。虽然用于构建这些级联的单个反应已经很好地建立起来，但在生产过程中将它们结合起来的能力将使有价值的类药物分子得以产生。C-X键形成反应的级联反应为杂环合成提供了巨大的潜力，因为它们引入了类药物分子中经常遇到的官能团和杂原子组合。级联序列涉及多达四个键形成过程，将用于在一个步骤中制备复杂的药物样分子。化学的一个重要方面包括证明它可以应用于阵列合成。

The chemistry in this proposal involves the development of a series of cascade processes based on combinations of C-N, C-O, C-S and C-C coupling reactions, mediated by copper and palladium based catalysts, to deliver a variety of functionalised heterocyclic products. Significant variation of the heterocyclic core and the nature and position of the substituents will be possible employing what is essentially a single strategy. Although the individual reactions used to construct these cascades are well established, it is the ability to combine them in productive processes that will allow valuable drug-like molecules to be produced. Cascades of C-X bond forming reactions offer great potential for heterocycle synthesis as they the introduction of the functional groups and heteroatom combinations frequently encountered in drug-like molecules. Cascade sequences involving up to four bond forming processes will be used to prepare complex, drug-like molecules in a single step. A significant aspect of the chemistry involves demonstrating that it can be applied to array synthesis.