The Lab Notes

Sodium formaldehydesulfoxylate,1 first reported in the chemical literature in 1905 and marketed as Rongalite (Figure 1, CAS: 149-44-0, dihydrate: 6035-47-8, from the French word rongeage for decolorize)- is a commodity chemical used in the textile and dye industry as a bleaching agent and as a reducing agent in redox initiator systems for polymer formation. Historically it has…

Dr John Studley, Science Director at Scientific Update and Dr Rachel Grainger from Astex Pharmaceuticals got together ahead of our forthcoming Organic Process R&D Conference in Lisbon, Portugal on 23-25 September. Q: Dr John Studley (JS) Can you give us an overview of Fragment Based Drug Discovery (FBDD) and how you see the technique evolving over the next decade? Dr…

Deoxyfluorination remains amongst the most frequently used method for preparing alkyl fluoro compounds.1 The reaction typically involves activation of a leaving group followed by SN2 (but occasionally SN1) reaction with fluoride ion. This is usually accompanied with significant elimination side-reactions and can frequently be low yielding. The original deoxyfluorination reagents such as DAST (diethylaminosulfur-trifluoride) and…

Dr John Studley, Science Director at Scientific Update and Dr William Goundry from Astra Zeneca got together ahead of our forthcoming Organic Process R&D Conference in Lisbon, Portugal on 23-25 September. Dr William Goundry Q: Dr John Studley (JS) We are looking forward to your presentation ‘The Good, the Bad and the Ugly! Successes and…

One of the most significant technological advancements in synthetic organic chemistry in recent years is the use of photoredox catalysis to generate synthetically useful radical intermediates and promote novel reactivity. It has the potential to enable exploration of chemical space that remains difficult to access using traditional synthetic methodology and too improve the efficiency of…

When I started my PhD one of my then colleges spent months trying to make something that was sitting on a shelf in the chemical store room less than ten feet from their bench. Could there really be anything more frustrating? Well yes there could. Imagine finding a new catalytic process or synthetic transformation only…

Scientific Update are delighted to sponsor 10 PhD students to attend and present their work at the '6th Winter Process Chemistry Conference' which takes place in Birmingham, UK | 9th-11th December 2019. More DetailsApplication Form

Aryl boronates are among the most widely used synthetic intermediates in the pharmaceutical and agrochemical industries, both in R&D and commercial manufacture.1 Historically these key building blocks have been made using transition metal (Pd, Cu, Ni) catalysed cross coupling reactions between an appropriate aryl halide (usually bromide,  iodide or activated chlorides) and an alkoyboron species.2 Efforts to…

Netarsudil- a ROCK kinase inhibitor marketed by Aerie pharmaceuticals as RhopressaTM- was recently approved by the FDA for ocular hypertension.1 An asymmetric synthesis is challenging due to the aryl group lowering the pKa of the α-hydrogen, rendering it very susceptible to racemization both during synthesis of the amino acid and subsequently amide coupling to an unreactive, poorly…

Dr John Studley, Scientific Director at Scientific Update recently spoke to Dr Boris Gorin, Eurofins Alphora, Toronto, Canada ahead of his presentation at the 2019 ‘Organic Process Research & Development’ Conference in Toronto, Canada. Boris will talk about “Eribulin Mesylate, a Journey from Synthetic Route Discovery to Scale-Up Manufacture”. John Studley (JS): Can you tell us a bit…