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A Mild Method for Dehydration of a Base-Sensitive Primary Amide- Toward a Key Intermediate in the Synthesis of Nirmatrelvir

Nirmatrelvir, the active ingredient of the Pfizer drug Paxlovid (Figure 1), is an inhibitor of the SARS-CoV-2 main protease enzyme.1 A key transformation- the final synthetic step in the synthesis of Nirmatrelvir- is dehydration of a primary amide (Figure 2).The amide starting material is prepared by reaction of the corresponding ester with ammonia.2 Various methods

Impurities – How Do You Combat Those Elusive Threats?

Many organic impurities, such as nitrosamines, are known to be harmful to human health. Therefore, regulatory bodies and government set strict limits to protect us all. Even in small quantities, pharmaceutical impurities can have serious negative health impacts and influence the behaviour and efficacy of a drug. Organic impurities fall into a number of categories.

One training course – Three different perspectives  

We spoke to chemists at different stages of their careers about their experiences of attending our ‘Chemical Development and Scale Up in the Fine Chemical and Pharmaceutical Industries’ training course. Ben Littler  Ben told us that he had taken the ‘Chem Dev’ course twice as an early career process chemist!  Both courses were held as

The Golden Age of Travel

What an experience to treasure! Claire and Hannah from Scientific Update Ltd were invited to travel on the beautiful British Pullman last week, for a specially hosted event ‘Golden Age of Travel with The Netherlands’. Passengers were encouraged to dress up in 1920’s costume and it certainly was a rather glamorous and special occasion. Everyone enjoyed fine

Now You See Me, Now You Don’t- a Judicious Work-Around for Over-Bromination at Benzylic Carbon

One of the most challenging reactions we carry out as synthetic chemists is bromination of a benzylic carbon- the so called Wohl-Ziegler reaction.1 It’s a seemingly simple transformation – not particularly difficult to perform- and potentially very useful. In fact it’s a little too easy. Just add NBS and a radical initiator to an aryl

Using Electrochemistry to Make Carbon-Carbon Bond Formation More Sustainable

Finding generally applicable, more sustainable, scalable methods to construct C-C bonds via cross-coupling is likely to be one of the major challenges that process chemists will face over the next decade. At the moment chemists overwhelmingly rely on pre-formed nucleophilic organometallics (such as Grignard, organozinc and organoboron reagents) in C-C couplings with an electrophile (such

Accelerating Reaction Development through Open-Source HPLC Data Analysis

Acquisition and processing of analytical HPLC data is often the main bottleneck when performing automated data-rich or high-throughput experimentation. Even though it was over 20 years ago, I well remember spending most of each day running, processing and compiling HPLC data when using an automated reaction platform to run 4 data-rich time course experiments in

Light, Camera, Action- Photoinduced Oxygen Transfer using Nitroarenes to Cleave Alkenes

When one thinks about the chemistry of alkenes, oxidative cleavage via ozonolysis will be close to the top of the list. Certainly in the top 5. Discovered by the Swiss chemist Friedrich Schönbein in 1839, this reaction remains -both academically and industrially- a highly efficient, sustainable method for introducing oxygen into both simple feedstock materials

PerFected Cubane

In the spring of 1940, John Archibald Wheeler, eminent theoretical physicist, called up his then PhD student, Richard Feynman (generally regarded as the most famous modern-age physicist) and said “Feynman- perhaps there’s only one electron in the Universe” a single entity moving backwards and forwards in time. If true it would be one hard working

Our Sadness on the Passing of Her Majesty The Queen

We are deeply saddened to hear of the passing of Her Majesty The Queen. She has been a constant in our lives and the only monarch we have known.  We would like to thank her for her dedicated service to her country and the Commonwealth for 70 years and send our heartfelt condolences to all

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