The Lab Notes

In my previous blog I referred to changes in learning models for industrial chemists described in an editorial in the Journal of Medicinal Chemistry by Dean G. Brown on ‘Adapting to the Changing Landscape of Biotech-Driven Drug Discovery’ (DOI: 10.1021/acs.jmedchem.3c02035) that I discovered through Derek Lowe’s ‘In The Pipeline’ blog titled ‘The Current Industry Landscape’…

Derek Lowe’s ‘In The Pipeline’ blog titled ‘The Current Industry Landscape’ on 27 Nov 2023 alerted me to an excellent overview editorial in the Journal of Medicinal Chemistry by Dean G. Brown on ‘Adapting to the Changing Landscape of Biotech-Driven Drug Discovery’ (DOI: 10.1021/acs.jmedchem.3c02035). One thing that struck me as I read both the blog…

If you are working in industry and are responsible for safety, how do you safely scale up a given chemical reaction? How do you tackle issues like heat transfer, gas release, exposure control, waste stream issues and more? The core of any process safety study is a correct description of both heat and gas release…

When I first started working as an industrial process chemist one of my more experienced colleagues told me that you can only really know how well a process performs until you run it on at least a 5 kg scale. I found that to be good advice but as I developed my skills in the…

Nitrous oxide- discovered by Joseph Priestley in 1772 and known affectionately as “laughing gas” - is now a class C drug in the UK under the misuse of drugs act 1971. Possession will be illegal by the end of 2023. If, However, you can get hold of some (or have some to get rid of)…

The resurgence of electrochemistry in medicinal chemistry laboratories has created the demand for the rapid delivery of up to a few kilograms of material by the same methods in order to quickly evaluate whether the candidate molecule is a viable clinical candidate or not. Electrochemical processes have been successfully scaled up to commercial scale using…

Single atom deletion and skeletal editing of complex organic molecules is an interesting and potentially very impactful area of research. Over 100 papers mentioning the term ‘skeletal editing’ have been published in the past 2 years. The ability to selectively add or remove a single heteroatom from a molecules core architecture is distinctly different from…

A well-written experimental protocol is one of the hallmarks of good process chemistry that we teach at Scientific Update in our Chemical Development course, so in this blog I thought I’d highlight an excellent example recently published in an open-access article by Nicholas Isley and Fabrice Gallou from Novartis (Helv. Chim. Acta 2023, 106, e202300143,…

A recent paper from a Dutch team brings together two items that have fascinated me since graduate school in a way that comes in the category of “I can’t believe nobody thought of that before!” (Chem. Commun., 2023, 59, 3838) The ability to upgrade the enantiomeric excess of a solid by recrystallization The use of…

Five-membered heterocyclic arenes account for a large portion of the heterocycles found in pharmaceuticals and bioactive molecules.1 Synthesis of heteroaryl halides and elaboration via metal catalysed cross coupling reactions- particularly with aliphatic amines- is, however, known to be challenging. These small heterocycles-particularly electron-rich systems- frequently coordinate to palladium, promoting catalyst deactivation via displacement of the supporting…