Vapourtec’s R-Series flow chemistry system has recently been cited in an important paper published in peer review journal Organic Process Research & Development by US firm Gilead concerning the synthesis of Remdesivir, an antiviral used to treat severe manifestations of the COVID-19 disease.
Remdesivir was originally developed by Gilead as an anti-viral treatment against the 2014 Ebola outbreak in Liberia. Recently, following positive results in accelerated trials, Remdesivir became the first COVID-19 treatment to receive a positive scientific opinion by the Medicines and Healthcare Products Regulatory Agency (MHRA).
In late May 2020, the Department of Health and Social Care approved Remdesivir as the first medicine to treat COVID-19 in the UK and it has become an important medicine in the global fight against the pandemic.
The paper, entitled “Development of a Large-Scale Cyanation Process Using Continuous Flow Chemistry en Route to the Synthesis of Remdesivir” (Tiago Vieira, Andrew C. Stevens, Andrei Chtchemelinine, Detian Gao, Pavel Badalov, Lars Heumann of Gilead Alberta ULC and California-based Gilead Sciences) describes the development of a continuous flow cyanation reaction from early lab trials to initial production quantities.
The R-Series system’s role in the research concerned the implementation of cyanation chemistry at initial laboratory scales and the application of a continuous process approach in mitigating the risk of handling large amounts of hazardous reagents as well as delivering better control of the reaction parameters.
Dr Manuel Nuño of Vapourtec commented: “The article published by Gilead’s team perfectly highlights the benefits of continuous flow chemistry and why most of our clients have an industrial profile.
“Reactions that are difficult to control, with hazardous reagents and/or intermediate species, are usually carried out in a controlled manner by working with small amounts. This becomes an apparent problem when the process is scaled up in batch as it requires greater amounts of hazardous reagents and a greater capacity for the cooling or heating a large vessel.
“For this reason Vieira et al looked at translating the process into a flow regime. With a much smaller reactor volume and the inherent ability of flow chemistry systems to deliver improved temperature control and mixing, this reaction was successfully carried out using our R-Series system.
“With an improved diastereoselectivity in flow and the key reaction parameters defined using the R-Series, the team at Gilead then scaled the process to a kilogram scale prior to commissioning a pilot plant in a reasonable time frame,” added Dr Nuño.
Gilead Sciences is a biopharmaceutical company, based in California, that researches, develops and commercialises drugs. The company focuses on antiviral drugs used in the treatment of HIV, hepatitis B, hepatitis C, and influenza.
Vapourtec MD and founder Duncan Guthrie: “This recent paper highlights how flow chemistry is playing a part in the manufacturing of treatments to tackle the coronavirus pandemic and demonstrates the versatility of the R-Series in delivering a cyanation process more effectively than a traditional batch approach.
“As pressure is put on the supply chain to deliver Remdesivir for the treatment of COVID-19 we expect to see a lot more of this molecule in flow. Lots of steps are hard to scale in batch,” he added.
The R-Series has already been cited in over 550 peer review publications making it, by a considerable distance, the most productive laboratory scale flow chemistry system in the market place.
To read the paper by Gilead click here