Toward beta-aminocarbonyl motifs and nitrogen-susbstituted aromatic heterocycles

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Over 90% of the compounds manufactured and tested by pharmaceutical companies have at least one nitrogen atom in their structure, and approximately one reaction out of six performed in the pharmaceutical industry involves the formation of a carbon-nitrogen bond. As such, new methods to access nitrogen containing molecules can help in drug discovery by providing shorter and more efficient access to these compounds. Many fine and bulk chemicals also incorporate nitrogen atoms. Surprisingly, the conversion of cheap petrochemicals or easily accessible starting materials (alkenes, alkynes and arenes) into nitrogen-containing molecules currently requires several steps and more cost-effective, efficient processes are possible and needed. Such direct processes stand out as highly desirable but remain rarely used in industry and academia, despite well-recognized potential and intense research efforts worldwide. This proposal will provide such new technology targeting common structural elements founds in pharmaceuticals and bioactive natural products: beta-aminocarbonyl motifs and nitrogen-substituted heteroarenes. This research will benefit from a close collaboration with AstraZeneca thus maximizing the potential of such new technologies as tools in pharmaceutical research and development and allowing the synthesis of scaffolds that could display interesting biological activities in the Central Nervous System (CNS). As part of this research, students will receive training that is ideally suited for future work in medicinal chemistry or fine chemicals sectors.