Imperial academic wins AstraZeneca prize in synthetic chemistry

Dr James Bull has been recognised for his work discovering faster, cheaper methods for producing molecules useful for drug discovery and development.

Dr Bull and his team’s methods for producing several molecules of interest for new drugs have been picked up by AstraZeneca (AZ) chemists, who nominated him for the award.

This is a very nice validation of the type of work that we are doing and highlights the crucial role of synthetic chemistry in drug discovery. Dr James Bull

One such method, for creating molecules called sulfoximines that are finding favour in potential new cancer drugs, has been quickly picked up by AZ chemists to produce large quantities of an already promising drug candidate.

The method is simpler, involving fewer steps, and avoids the use the extremely expensive metal rhodium, making the process cheaper. A more efficient process also means the process is greener as it uses less energy.

Dr Bull, from the Department of Chemistry, said: “I am both surprised and delighted to receive this prize. There was no application, but it was chosen by AZ scientists. This is a very nice validation of the type of work that we are doing and highlights the crucial role of synthetic chemistry in drug discovery. I am very grateful to the students and collaborators I have worked with.”

As part of the prize, Dr Bull will give a lecture about his group’s work at the third annual conference New Frontiers in Synthetic Chemistry, organised jointly between the Royal Society of Chemistry and AstraZeneca.

Rapid impact

Synthetic chemists like Dr Bull develop user-friendly, simple methods for producing molecules with certain arrangements of atoms that could be useful to medicinal chemists, who design potential new drug molecules.

Developed in collaboration with a team in Italy, the team’s new method for producing sulfoximines not only reduces the synthesis steps for mass production, as with the AZ cancer drug candidate, but also allows other potential drugs that contain sulfoximines to be more easily produced in academic and industrial labs.

This wide use is important, says Dr Bull, as methods for producing molecules should be scalable – they should be able to produce milligrams of the compound for testing as well as kilograms for manufacture.

He said: “New synthetic methods have the potential to be readily adopted and generate rapid impact in improved synthetic routes, as well as to influence the types of compounds that can be prepared. I was also particularly excited to see our work on sulfoximine synthesis used on large scale.”

Academia meets industry

Jeremy Parker, executive director of early chemical development at AstraZeneca, said: “New synthetic methodology is at the heart of our efforts to explore novel chemical space, as we look to construct structurally diverse molecules. These types of molecule are helping us tackle targets that have been previously described as undruggable.

“The close relationship with UK academia allows us to use their expertise as we look to make new molecules and help with the serious challenge of applying the methodology on kilogram, and potentially tonne, scale.”

The Imperial team also works on methods for creating ring-shaped molecules called heterocycles that may be useful to drug developers. This includes new methods for attaching different components to the rings to incorporate new features.

The researchers are also increasingly working with automated processes and optimisation of reaction steps, and the team are involved in Imperial’s new Centre for Rapid Online Analysis of Reactions (ROAR).

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