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Convergent and Efficient Synthesis of Novel Heteroaromatics

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New ways to make important chemicals

New research from an EU group is providing new preparative methods for a wide range of azoles, chemical compounds with a ring structure that are of great importance in the pharmaceutical industry.


Azoles are important building blocks of countless complex chemicals. Some members of the azole family are usually created through achemical reaction called a [3+2]-cycloaddition. However, for most of the azole family this attractive approach cannot be used as one of the required components of this reaction is highly reactive, making the reaction inefficient and thus, expensive. The EU-funded SYNHET (Convergent and efficient synthesis of novel heteroaromatics) project aimed to create a more general [3+2]-cycloaddition strategy to create a wider range of azoles. To achieve this, the project exploited a recent discovery by one of the research partners where a different, more stable precursor could be used. SYNHET focused on refining this new [3+2]-cycloaddition strategy. This resulted in a process that used less catalyst and less starting material, while still remaining efficient. The project identified a number of new compounds that can be used as precursors. Researchers also showed that using the new method, the two precursors could be joined in different orientations, creating a host of new azoles. Finally, SYNHET used this methodology to produce a number of novel azoles at practical scale to demonstrate its applicability. The work of this project can ultimately lead to new and cheaper pharmaceuticals and bio-based chemical products.


Azoles, chemical compounds, [3+2]-cycloaddition, reaction, catalyst

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