Direct methods for the preparation of heterocycles and bis-heteroaromatics

在这个项目中，我们将开发基于试剂的新方法，以提供简单、可靠和高度实用的合成方法，在有机合成中具有广泛的适用性。N-甲基-O-对甲苯磺酸基羟胺将为醛和酮的直接转化提供一种新的方法，当这些化合物直接与多种双杂核亲核剂原位反应时，将提供一锅反应序列来获得各种具有生物意义的杂环。N-甲基-O-苯甲酰羟胺(及其类似物)与芳基卤化物的Buchwald偶联反应将导致级联反应序列，从而提供直接获得双官能化杂芳烃的途径，这些杂芳烃存在于各种具有生物重要性的合成和天然化合物中。将这些新方法应用于靶向化学阵列的制备，将为生物分析提供一系列密集功能化产品的途径。

Within this project we will develop new reagent based methodology to provide simple, robust and highly practical synthetic methods of broad applicability within organic synthesis. N-Methyl-O-tosyl hydroxylamine will provide a new method for the direct conversion of both aldehydes and ketones to alpha-oxysulfonyl carbonyl compounds, which, when treated directly with a variety of bis-hetero nucleophiles in-situ will provide a one-pot reaction sequence to access a variety of biologically significant heterocycles. Buchwald coupling of N-methyl-O-benzoyl hydroxylamine (and analogues) with aryl halides will lead to a cascade reaction sequence to provide direct access to bis-functionalised heteroaromatics which are present in a wide variety of both synthetic and naturally occurring compounds of biological importance. Application of these new methods to the praparation of targeted chemical arrays will provide access to a series of densely functionalised products for biological assay.