MEMBER NEWS
SCI NEWS
Give us your opinions
As part of SCI’s goal to improve your membership experience, our newly- formed Membership Committee is launching a survey to help us further understand the interests and concerns of our members. This new committee was created over the summer with the important and distinct role of helping SCI improve the way it serves the needs of its members. The committee has many things to focus on over its first three-year term, but the most important is to understand why you all became members, what you have enjoyed doing, and what you would like to see SCI do in the future. After all, without you, SCI would not exist. On this, we would like your help. The
Membership Committee has written a short survey asking about some of the more significant activities and services that SCI provides. We ask that you give us 10 minutes
of your time to answer these few questions. The survey can be found at:
bit.ly/SCIMem2017, and we will announce in due course when you can expect the headline findings from the survey to be published. We hope that with your participation in this survey, we will be able to help bring even more value to SCI membership. Of course, we don’t expect you to do
this for nothing. That is why in return for your support in completing this survey, everyone who completes the survey and provides their name and email address will receive a £10 discount for any SCI conference taking place before the end of 2019, and will be entered into a prize draw for complimentary attendance at any one-day SCI event in 2018-19. We hope to see you all at one of those events soon. There will also be opportunities
to become more involved with our Membership Committee and its activities, as plans progress – watch this space!
SCI SCOTLAND GROUP COMPETITION
The bridge between learning and industry
Katherine Geogheghan, a PhD student at the University of Edinburgh, is another winner of this year’s Where science meets business competition, run by the SCI Scotland Group. Entrants wrote an article outlining their PhD research and how it is important to industry. This is Geogheghan’s article Suzuki-Miyaura: Linking academia and industry
Mechanistic chemistry can bridge the gap between academia and industry, allowing the rational design, optimisation, and scale-up of new chemical reactions. Cross-coupling has become an essential tool for organic synthesis, with the ability to form a new carbon-carbon bond now used extensively throughout discovery chemistry in the pharmaceutical, materials, and agrochemical sectors. The pioneer chemists who developed cross-coupling into the key reaction it is today are Heck, Negishi, and Suzuki. The impact of their research in ‘palladium-catalysed cross-couplings in organic synthesis’ has become so significant that they became Nobel Prize laureates in
2010, giving chemists the ability to form
more new and complex molecules than ever before.
Katherine Geogheghan
Many ‘blockbuster’ drugs contain
biaryl moieties, including Lipitor from Pfizer, which made a record $130 billion over 15 years.
The Suzuki-Miyaura reaction was originally reported in 1979 and since then the use of this reaction has continued to grow, resulting in it becoming the most widely utilised tool for catalytic carbon-carbon bond formation. The palladium catalysed coupling of a boronic acid and an organohalide compound is used greatly throughout the pharmaceutical industry, and three decades later we are still working to further improve and understand this complex reaction. The need to improve is obvious. It allows higher yields, milder conditions,
and more diverse products. Recent developments now allow the coupling of previously challenging substrates, and reactions can be performed at lower temperatures and with lower catalyst loadings – reducing the cost and increasing the scope of this powerful reaction. But without a full understanding of the mechanism, improvements can only take us so far. The mechanism of the Suzuki-
Miyaura reaction continues to be an area of controversy. While the use of boronic acids has been widely studied, there are still problems left unsolved. Boronic acid derivatives are used as replacements for unstable boronic acids in order to mitigate undesired side reactions, but very little is known about the mechanism by which these species react. Whether they can cross-couple directly or need to undergo pre-activation remains unknown. My research aims to elucidate the mechanism of this cross-coupling process. This in-depth understanding could be directly implemented industrially to improve the scale up process for chemical synthesis and has two major advantages, not only producing more desired product but giving a reduction in waste side products, which cost time, money, and energy to separate and dispose of. This insight would also aid discovery chemistry, in which carbon-carbon bond construction is frequently carried out using cross-coupling reactions. A key example of where this
knowledge would be beneficial is in the synthesis of a crizotinib, a tyrosine kinase inhibitor – a treatment for advanced lung cancer. Tyrosine kinases are enzymes that can stimulate cancer cells to grow. Pfizer achieved large scale synthesis of this complex molecule using the Suzuki-Miyaura coupling of a boronic acid derivative, but we still don’t fully understand the mechanism. This missing information could help to minimise unwanted side products and increase conversion to the desired product, which could go on to save lives. My research directly addresses this
challenge, to fill this void in knowledge which bridges the gap between academia and industry.
48 09 | 2017
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