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Transition metal catalysis in vivo-cisplatin-mediated tertiary amide prodrug activation of cytotoxic agents in cancer cells

Figure: 1 The idea of using transition metal chemistry in a cellular setting might at first seem counterintuitive- biological conditions are challenging with respect to stability, efficiency and catalyst (not to mention patient) poisoning. Having said that many important intracellular processes are modulated by transition metals complexed in metalloproteins, with functions including storage and transport

Intrinsically safe and shelf stable diazo transfer reagent for fast synthesis of diazo compounds

At the Scientific Update OPRD conference in Milan earlier this month, Xiaohu Deng from Kura Oncology discussed a pyrimidine-derived diazo intermediate that exists predominantly in the tautomeric ‘tetrazole’ form at equilibrium in solution.[1] The compound was shown as a putative retrosynthetic building block for synthesis of a J&J P2X7 antagonist (Figure 1).[2] I’d not come

You really wouldn’t have wanted to get sick in the 1900’s…..

Antibacterial chemotherapy before the turn of the nineteenth century really was a brutal business. A fine line between killing bacteria or the host organism- the human population. Mercury and bismuth based ointments and elixirs were available from apothecaries and administered by quack doctors as remedies, most notably for syphilis- a sexually transmitted bacterial infection caused

Antibiotics, synthetic organic chemistry and the war against the microbes:

One of the first encounters I had with complex structures and challenging organic synthesis was a course I took on the synthesis of antibiotics as an undergraduate chemist at Bath university almost thirty years ago. These molecules and I had had a love hate relationship for much of my early childhood, having consumed what must

New Award for Women in Chemistry

I am delighted to share with you the announcement of a new award and a ‘call for nominations’. The ‘1st Dr Margaret Faul Women in Chemistry Award‘ is intended to recognize and highlight outstanding contributions by young women to research in organic chemistry. The prize provided by Thieme includes an award of € 5,000. For more

John Studley to join Scientific Update as Scientific Director

Scientific Update is delighted to announce the appointment of Dr John Studley, formerly Head of Process Chemistry for Vertex Pharmaceuticals, UK. John will join the team at Scientific Update in August 2018 as Scientific Director bringing over 20 years’ experience in drug discovery, process chemistry and scale up, having previously worked for Rhone-Poulenc, Oxford Asymmetry and Vertex

OPRD US 2018 Conference

We had a fantastic turn out for our #OPRDUS18 Conference in Clearwater, Florida last month. It was great to see our speakers, exhibitors and attendees and the feedback we received was excellent. Thank you for coming along! Our Technical Director Dr Will Watson opened the conference and we invited Dr Paul Murray and Dr André de

Are you using DoE to its full potential?

Where can DoE fit in process development? Are you using DoE to its full potential? A common misconception with experimental design in chemistry is that its use comes once a process had been planned and tested, just before commercialisation. In fact, DoE is arguably more useful at the start of a process for efficiently screening

Why does the management of impurities scare people?

A recent survey suggested that out of all CMC topics the one at the forefront of many people’s minds and concerns is that of impurity control.  Why might that be the case? After all there is a strong framework provided by ICH in the form of ICH Q3A / Q3B (Impurities in drug substance and

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