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Two New Reactor Types for Rapid Electrochemistry Scale-Up

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

Less is More- Deletion, Insertion and Everything In-Between

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

The Value of a Good Experimental Write-Up

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 New Application for a Classic Piece of Apparatus

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

These Are Tri(azol)ing Times…. Great Chemistry- But Do Not Attempt on a Damp Day

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

One Functional Group, So Many Functions

The complex machinery required to take a drug through development and regulatory approval can be as arduous as the discovery of the molecule itself. In recent times the demand for COVID-19 drugs has added to the pressure to expedite this process in record time and several organizations working in the small molecule arena have met

Not a Dry Eye in the House

Yesterday I glanced through the list of drugs approved by the FDA in Q2 2023. One in particular, Miebo,1 -developed by Bausch and Lomb- made me sit up and stare. The compound is a partially fluorinated alkane (1-(Perfluorohexyl)octane, Figure 1) and is administered directly into the eye as a neat, anhydrous liquid to treat dry

It Ain’t Easy Being Green

One of my recent bugaboos has been the increase in the number of papers claiming a “green” synthesis, reagent, process or solvent. It seems that I am not alone in my concerns of the misuse of words such as “green” and “sustainable” based on a recent paper called ‘What does it mean that “something is

Hey Phenol- Everyone has their Cross to Bear

Tert-butyl phenols are important commodity chemicals, with annual production exceeding 120,000 t per annum. They have multiple industrial applications including agrochemicals, antioxidants- in particular 2,6-di-tert-butyl-4- methylphenol (BHT, Figure 1), foods, flavours and fragrances and pharmaceuticals.1 BHT in particular, used as an antioxidant in polymers and oils and prepared by reaction of p-cresol with isobutylene in

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