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

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

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

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

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

A number of years ago, during a scale-up campaign, I worked to try and convert a relatively simple, high-yielding Suzuki coupling from a relatively standard set of homogeneous coupling conditions to heterogeneous conditions using a palladium on carbon (Pd/C) catalyst. The reason for making the change was that although the homogeneous conditions worked very well,

The Scientific Update Ltd team recently worked with an amazing group of women to run the first ‘Empowering Women In Organic Chemistry Europe‘ Conference and it was fantastic to read all the positive reviews after the event. It was such an enriching and rewarding day full of positivity. Everyone who participated was totally open and

A couple of weeks ago I attended the 20th annual Bristol Synthesis Meeting at the Victoria rooms in Bristol, UK.1 Always an excellent event, and this one was no exception. I was intrigued by a presentation given by Franziska Schoenebeck from the University of Aachen, Germany on the application of organogermanes in cross coupling chemistry.

Biocatalysis has the potential to transform how process chemists make molecules, both in terms of improving existing routes to be more sustainable, and to enable shorter new routes via transformations not feasible using chemical methods. A recent review by a team at Pfizer (S.P. France et. al. JACS Au 2023, 3, 715-735) gives an excellent