Diels-Alder/Ene Reactions for the Multi-Component Synthesis of Natural Product Inspired Bioactive Chemical Libraries

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Despite the many fantastic advances in health treatment over the past 50 years new drug molecules are always needed. Sometimes this is to combat existing health problems for which a solution is yet to be found, such as some cancers, and sometimes this is to deal with emerging problems, such as the rise of drug resistant bacteria (e.g. MRSA). Modern drug discovery relies on chemists to make new molecules for testing as potential drugs which can be then optimised to for use by a patient. However current approaches to this problem can be very time consuming and inefficient. The inefficiency of these processes also results in the creation of large quantities of chemical waste which can in turn cause environmental problems. This project aims to find a solution to this through the use of one-pot chemical reactions where, in place of sequential chemical transformations (one after the other), several can happen in the same reaction flask. This efficient approach leads to a vast reduction in the waste generated, whilst at the same time increases the number of different molecules a chemist can make in a day and thus the number of molecules which can be tested. Making many molecules, rapidly and with a reduction in waste can only help to speed up the drug discovery process.Specifically this project will develop new one-pot methods to make a library of very different molecules, very quickly. The molecules we will target have the potential to be new anticancer or new antibacterial agents, so will also test these molecules as lead compounds for treatment of these diseases.