The Lab Notes

The count down has begun and we only have one month to go now until we come to New Orleans for our '47th Organic Process R&D Conference' on 22-24 June. We are so excited about holding this face to face event in such a vibrant brilliant location!  The 3 day meeting will include 16 presentations…

Scientific Update to Welcome New Technical Associate for North America & Asia Pacific - Dr Ben Littler Scientific Update is delighted to announce the appointment of Dr Ben Littler, formerly Executive Director  Process Chemistry for Vertex Pharmaceuticals. Ben will join the team at Scientific Update in August 2022 as Technical Associate, North America & Asia…

Phenols and anilines are two of the most important building blocks in industrial chemical manufacturing. Any process capable of converting one into the other is going to generate a lot of interest, and a paper by Shi and co-workers does just that.1 Direct conversion of an aniline to a phenol is a relatively straightforward transformation…

Process chemists at Genentech recently published their work on development of a kilo-scale synthesis of JAK-1 inhibitor- GDC-4379 (Figure 1).1The central heterocyclic core of the molecule consists of a 4-aminopyrazole moiety (elaborated as the pyrazolopyrimidene amide- presumably the inhibitor hinge binding fragment in the kinase active site) with an additional aryl substituent at C-3 and…

Oxidation of allylic alcohols to enones, although on paper a simple reaction, usually requires insidiously toxic metals or metalloids such as chromium and selenium or hazardous peroxy- reagents.1 Scale-up of these methods remains particularly challenging. A team from GSK found themselves in precisely this position when developing a synthetic route to a steroid-derived HIV maturation…

The importance of methylation in the discovery and development of bio-active small molecules is well known. I presented a webinar a couple of years ago on the “The magic methyl in medicinal chemistry,” demonstrating the unique properties of this, the simplest functional group.1 I also reviewed the state of the art in synthetic approaches to…

Perhaps the best-known ring-expansion reaction is the Baeyer-Villiger oxidation, first reported in 1899- not surprisingly by Adolf von Bayer and Victor Villiger. As we’re all aware, reaction of a carbonyl with a peracid generates a Criegee-type intermediate that undergoes rate-limiting concerted rearrangement to form an ester or lactone. The migration order is substituent dependant, with…

The first electrophilc aromatic substitution reaction you were taught as an undergraduate was almost certainly nitration.1 Nitration and subsequent reduction of the aryl nitro group to an aniline via high temperature metal catalysed hydrogenation remains an important industrial process. The reduction has many flavours- both in terms of the substitution pattern on the aryl (and…

The ability to handle gaseous reagents presents a number of challenges for synthetic chemists. The problem becomes particularly acute when scaling up biphasic (liquid/gas) or even triphasic (gas/liquid/solid) systems due to limiting mass transfer effects. Pressure vessels or autoclaves are also not always practical and easy to come by. A practical solution to this (if…

To celebrate International Women's Day 2022  - Helen Spencer (Consultant BDM and Marketer) asked Scientific Update Ltd joint owners and Directors Dr Claire Francis and Hannah May - a few questions about their career journey. Q: Do you think it is important to celebrate International Women's Day? A: CF: Yes, for me it is an…