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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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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 READ MORE |
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8th Winter Process Chemistry Conference |
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Date: 05 December 2022 - 07 December 2022 Time: 12.30 noon - 4.30pm Location: Newcastle, UK |
16th Winter Conference on Medicinal & Bioorganic Chemistry |
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Date: 29 January 2023 - 02 February 2023 Time: 16:00 | Sunday 29th January, 2023 - 21:00 | Thursday 2nd February, 2023 Location: Steamboat Springs, Colorado |
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Chemical and Process Safety for Development Chemists |
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Date: 17 October 2022 - 25 October 2022 Location: Online Platform |
How to Develop Organometallic Catalytic Reactions in API Synthesis: Short Course |
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Date: 01 November 2022 - 03 November 2022 Location: Online Platform |
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Synthetic Approaches to the New Drugs Approved in 2022 |
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Date: 26 January 2023 Time: 15:00 (GMT), 16.00 (CET), 10.00 (ET), 7.00 (PT) |
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