SELECTIVE CATALYTIC FUNCTIONALIZATIONS

在药物化学领域，继续需要新的 高选择性的合成转化。由于酶制剂 反应通常表现出良好的选择性，我们一直在 有兴趣开发仿生反应，模仿 酶转化的风格，我们希望，他们的 有效性。 1.了解可以绑定和交付的模板类型 自由基转化为特定的氢原子。我们的发现是氮气 杂环化合物的使用开辟了一个新的领域。2.学习如何 生成C-O、C-F和C-N键。它们具有重要的意义 在药物化学方面。3.催化量的使用 模板分子。通过使用离子配对，氢键， 金属配位，或我们计划生产的分子络合 催化剂和底物之间的暂时缔合。4. 介绍了基质和基质之间的多重相互作用 试剂。应该会大大提高选择性，包括 对映体选择性。5.选择的功能化 柔性分子。多个交互可能会使 否则就是杂乱无章的衬底。6.EVEN的功能化 活性较低的C-H键。有了适当的定位，我们应该 能够使几何图形成为控制攻击的唯一因素 凶猛的试剂。7.对以下类型的概括 可以几何定向的变换。尤其是 吸引人的是金属卟啉催化的发展 化学，包括细胞色素P-450的氮类似物 我们最近发现的模型系统。8.使用 用于关联和设计模板的分子建模技术- 定向反应。

Within medicinal chemistry there continues to be a need for new synthetic transformations with high selectivity. Since enzymatic reactions typically exhibit good selectivities, we have been interested in developing biomimetic reactions which imitate the style of enzymatic transformations and, we hope, their effectiveness. 1. Understanding the types of templates that can bind and deliver free radicals to specific hydrogens. Our discovery that nitrogen heterocycles can be used opens up a new area. 2. Learning how to make C-O, C-F, and C-N bonds. They are of significant importance in medicinal chemistry. 3. The use of catalytic amounts of template molecules. By the use of ion pairing, hydrogen bonding, metal coordination, or molecular complexing we plan to produce temporary associations between catalysts and substrates. 4. The introduction of multiple interactions between substrate and reagent. Greatly increased selectivity should result, including enantioselectivity. 5. The selective functionalization of flexible molecules. Multiple interactions can immobilize an otherwise disordered substrate. 6. The functionalization of even less reactive C-H bonds. With appropriate orientation, we should be able to make geometry the only factor governing attack by a ferocious reagent. 7. Generalization of the types of transformations which can be geometrically directed. Particularly attractive is the development of metal-porphyrin catalyzed chemistry, including a nitrogen analog of the cytochrome P-450 model system which we have recently discovered. 8. The use of molecular modelling techniques to correlate and design template- directed reactions.