📣 Help Shape the Future of UKRI's Gateway to Research (GtR)

We're improving UKRI's Gateway to Research and are seeking your input! If you would be interested in being interviewed about the improvements we're making and to have your say about how we can make GtR more user-friendly, impactful, and effective for the Research and Innovation community, please email gateway@ukri.org.

Accelerated Synthesis of Agrochemicals and Pharmaceuticals (ASAP): Bridging the Gap Between Research and Application

Lead Research Organisation: University of Nottingham
Department Name: Sch of Chemistry

Abstract

Food and healthcare are the foundations on which our current quality of life is built. The pressure on these resources will only increase as the UK population ages, the global population reaches 9 billion in 2050 and the worst effects of climate change begin to manifest. Now more than ever, new medicines and agrochemicals will be vital in combating the growing and evolving threats that face society. A major challenge to the development of new medicines and agrochemicals is the high attrition rate of the candidate molecules being investigated, which drives up the financial cost, environmental impact and time associated with bringing a new product to market. Methods that allow rapid cost- and resource efficient preparation of desirable candidate molecules are therefore extremely valuable.

This programme will deliver a suite of synthesis methods to streamline the discovery and development of the next generation of agrochemicals and pharmaceuticals. Building on our recent discovery, we will develop new ways of making valuable molecular architectures while minimising the number of chemical operations required and avoiding the use of toxic or precious elements. By working in close collaboration with leading innovators in crop protection (Syngenta) and human healthcare (AstraZeneca, Pfizer and Carbometrics), we will ensure that our methods will be of direct and immediate benefit. We will also seek to make the reagents we develop commercially available, thus further enabling the rapid and barrierless uptake of our methods.

Publications

10 25 50

publication icon
Joynson B (2023) Skeletal Editing: Interconversion of Arenes and Heteroarenes in Helvetica Chimica Acta

publication icon
Ruffell K (2022) Umpolung Synthesis of Pyridyl Ethers by Bi V -Mediated O-Arylation of Pyridones in Angewandte Chemie International Edition

Related Projects

Project Reference Relationship Related To Start End Award Value
MR/V022067/1 01/03/2022 30/07/2025 £1,390,804
MR/V022067/2 Transfer MR/V022067/1 30/07/2025 29/07/2029 £0
 
Description We have developed synthesis methods based on non-toxic bismuth which enable the efficient preparation of new molecules that have potential applications in drug discovery or agrochemical development. These methods include:
- streamlined synthesis of 2-arylcyclohexadiones, which are an important motif in herbicides. Our method has the potential to replace traditional processes based on toxic lead/mercury reagents.
- streamlined synthesis of aryloxypyridines, which are an important substructure of several anticancer drugs.
- introduction of new chemical reactivity that formally overturns a traditional selectivity dogma.
- development of a new tool for monitoring the progress of reactions, with potential applications in safer / more efficient manufacturing.
- development of a method for chemically 'upgrading' lignin-derived biomass feedstocks into more valuable molecules.
Exploitation Route Our contributions to dione and pyridone arylation may allow agrochemical / pharmaceutical discovery chemists to make new molecules more quickly and more efficiently, thereby expediting development of the next generation of medicines and crop-protection products. Our work on reaction monitoring has received interest from the pharmaceutical and commodity chemicals sector as a low-cost method for following chemical processes, which complements existing methods.
Sectors Chemicals

Healthcare

Manufacturing

including Industrial Biotechology

Pharmaceuticals and Medical Biotechnology

 
Description One of the methods developed in our lab has been applied by an agrochemical company to prepare new molecules for field testing.
First Year Of Impact 2023
 
Title CCDC 2171727: Experimental Crystal Structure Determination 
Description Related Article: Katie Ruffell, Stephen P. Argent, Kenneth B. Ling, Liam T. Ball|2022|Angew.Chem.,Int.Ed.|61|e202210840|doi:10.1002/anie.202210840 
Type Of Material Database/Collection of data 
Year Produced 2022 
Provided To Others? Yes  
URL http://www.ccdc.cam.ac.uk/services/structure_request?id=doi:10.5517/ccdc.csd.cc2bwvqt&sid=DataCite
 
Description Computational Bi Collaboration 
Organisation Colorado State University
Country United States 
Sector Academic/University 
PI Contribution We provided experimental results and expertise of the research field.
Collaborator Contribution Expertise in computational modelling
Impact 10.1002/anie.202212873
Start Year 2021