Stereospecific arylation of organolithiums: synthetic, mechanistic and structural investigation

用于药物、农用化学品、香料等的新小分子的发现依赖于简单前体的可用性，这些前体可以被结合到更复杂的目标分子中。我们提出的研究将导致一种简单而有效的方法，使目前被认为难以甚至不可能获得的某些类别的分子，这一限制意味着一些潜在的目标群目前不可用。它寻求开发一种转化，在这种转化中，芳香环与含锂碳原子结合，从而使起始材料的形状在产品中被记住。这些产品具有一个共同的特征，即高度受阻的碳原子带有O、N或S取代基--这一特征很难用现有方法构建。所提议的反应是通过一个显着的机制进行的，通过合成有机化学家和结构无机化学家的联合研究，我们建议理解反应为什么是这样进行的，并利用这一理解来发展进一步的相关转化。

The discovery of new small molecules for use as drugs, agrochemicals, fragrances etc. relies on the availability of simple precursors that can be incorporated into more complex target molecules. The research we propose will lead to a simple and efficient way of making some classes of molecule currently considered difficult or even impossible to obtain, a limitation which means that some groups of potential targets are currently unavailable. It seeks to develop a transformation in which an aromatic ring becomes bonded to a lithium-bearing carbon atom in such a way that the shape of the starting material is remembered in the product. The products have the common feature of a highly hindered carbon atom carrying an O, N or S substituent - a feature difficult to construct by existing methods. The proposed reactions proceed by a remarkable mechanism, and by joint investigation involving both synthetic organic and structural inorganic chemists we propose to understand why the reaction works the way it does and to use this understanding to develop further related transformations.