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各种复杂的小分子。与这一努力相一致，我们的研究小组建立了一系列快速构建高价值有机化合物的化学过程。我们的新策略使用铜中间体或催化剂，从稳定和丰富的前体(芳基硼酸和羧酸衍生物)形成碳-碳键。异常温和的条件是通过环境空气中的氧气原位再生铜促进剂。这一新方法已被用于制备多功能化学构件和使药物分子多样化。为了确保商业合作伙伴采用该方法，并扩大我们的知识产权版图，我们的目标是：1)在合成与药物相关的分子子结构中展示这种方法；2)确认该过程的可扩展性/稳健性，以提供数十克到数百克的产品；3)确定能够在减少金属负载量的情况下提高反应性和范围的新催化剂；4)进一步发展与制药/定制合成/化学品制造领域的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.