Copper-catalyzed oxidative carbon-carbon bond forming processes

制药和精细化工部门必须以资源高效的方式制备多样、复杂的小分子。与这一努力相一致，我们的研究小组已经建立了一系列快速构建高价值有机化合物的化学工艺。我们的新策略使用铜介质或催化剂从稳定和丰富的前体（芳基硼酸和羧酸衍生物）形成碳-碳键。特别温和的条件是使铜促进剂在环境空气中的氧气就地再生。这种新方法已被用于制备多功能化化学构件和使药物分子多样化。为了确保商业合作伙伴接受这一过程，并扩大我们的知识产权范围，我们的目标是：1)在药学相关的分子亚结构的合成中展示这种方法；2)确认流程的可扩展性/稳健性，以交付数十至数百克的产品；3)确定新的催化剂，以提高反应性和减少金属负载的范围；4)进一步发展与制药/定制合成/化学制造领域合作伙伴的合作和许可关系。

The pharmaceutical and fine chemical sectors must prepare diverse, complex small molecules in a resource efficient manner. Consistent with this endeavor, our research group has established a series of chemical processes for the rapid construction of high-value organic compounds. Our novel strategy forms carbon-carbon bonds from stable and abundant precursors (aryl boronic acid and carboxylic acid derivatives) using a copper mediator or catalyst. Exceptionally mild conditions are enabled by the in situ regeneration of the copper promoter by oxygen in ambient air. This new methodology has been used to prepare polyfunctionalized chemical building blocks and to diversify drug molecules. In order to ensure uptake of the process by commercial partners and to expand our IP landscape we aim to: 1) demonstrate this method in the synthesis of pharmaceutically relevant, molecular substructures; 2) confirm the scalability/robustness of the process to deliver tens to hundreds of grams of product; 3) identify new catalysts that promote improved reactivity and scope at reduced metal-loadings; 4) further develop collaboration and licensing relationships with partners in the pharmaceutical/custom synthesis/chemical manufacturing sectors.