Cross-Coupling Reactions Leading to Chiral Heterocyclic Scaffolds for Drug Development and Manufacturing

杂环是至少含有一个非碳原子的环状分子，由于其良好的物理和化学性质，在药物发现和开发中被广泛使用。吡啶是FDA批准的药物中使用最广泛的芳香族杂环，对它们及其衍生物的制备方法的需求持续存在。不幸的是，大多数方法使用苛刻的反应条件，因此不能广泛使用。我们设计了一种概念上的新方法来制造吡啶衍生物，使用特别温和的条件，可以容忍广泛的官能团。这些反应还提供了直接接触小分子的途径，这些小分子具有类似药物的性质，而且很难通过其他方法制造出来。最后，我们的方法是催化的，因此将有助于降低药物发现和开发的环境成本。因此，拟议的研究将对寻找新的治疗剂产生直接影响。

Heterocycles, cyclic molecules with at least one non-carbon atom, are widely used in drug discovery and development due to their favourable physical and chemical properties. Pyridines are the most widely used aromatic heterocycle in FDA approved drugs and there is a continued demand for methods to prepare them and their derivatives. Unfortunately, the majority of methods to do this employ harsh reaction conditions and are therefore not widely useful. We have devised a conceptually new approach to make pyridine derivatives using exceptionally mild conditions that tolerate a wide range of functional groups. These reactions also provide immediate access to small molecules that possess 'drug-like' qualities and that are hard to make by other means. Finally, our methods are catalytic and therefore will contribute to the reduction of the environmental costs of drug discovery and development. As a result, the proposed research will have a direct impact on the search for new therapeutic agents.