From the beginning of the project we have been working towards the development of novel methods to provide access to meta-functionalized of fluoroarenes, aryl alkyl arenes and acetals in a more sustainable manner compared to the current methods. Our work is based on the introduction of carboxylic acids from CO2 to the substrates to direct the functionalization prior to the release of the carboxylic acid as CO2. Methods for the meta-arylation and meta-olefination of fluoroarenes and aryl alkyl ethers and acetals have been successfully developed. We have demonstrated that these methods tolerate many functional groups in most positions of the aromatic rings, being electron-donating and electron-withdrawing groups compatible with the methods. Also we have been able to develop a synthetic route towards a γ-secretase inhibitor, currently under testing for Alzheimer’s disease treatment by putting our method into use. This new synthetic route accelerates the previously patented route for the target compound.
We have started the dissemination of the results of this project, and we have recently published a review article in the chemistry journal Chemical Communications on the use of carboxylic acids as traceless directing groups that summarizes the background of the funded project. The results of this project will be submitted for publication in a leading scientific chemistry journal in the near future. The beneficiary has presented the results of the project at the Sheffield Hallam University where he was invited to deliver an oral communication. Prof. Igor Larrosa will present the results in conferences, talks in research and industry, as appropriate.
