New Discount Available for Andrew Teasdale’s Book, ‘Mutagenic impurities’ click on the image below for more details. Andrew Teasdale is a senior principle scientist within AstraZeneca, with 25 years experience in the industry. Andrew is also the inventor of the purge factor concept applied to the risk assessment of mutagenic impurities. Over the last 10
Month: February 2023
Several weeks ago I did my annual analysis of the synthetic routes used to prepare small molecule drugs approved by the FDA in the preceding year, obviously in this case 2022.1 I hope those of you who have seen the presentation found it as interesting to watch as I found to put it together. One
Almost Two Centuries Later, Functional Group Tolerant Conditions Identified for the Electrochemical Kolbe Coupling!
Two principles that we at Scientific Update teach in the foundational “Chemical Development” course are that new experimental methods can open new opportunities for old reactions, and that as scientists we should be looking to understand the mechanisms of empirical observations. Both of these principles are exemplified in by a recent pre-print publication by the
“How many steps are there in a synthetic route?” is one of the foundational questions for any chemist, but as with many apparently simple questions, the answer isn’t always that simple. In many cases chemists are incentivized to give an artificially low step count because it makes their new route look better and therefore more
Love it or hate it, triphenylphosphine oxide (TPPO, Figure 1) is something we all encounter at some point during our chemistry careers. Most of the time it’s just a by-product from well-established and widely used process such as the Mitsunobou, Wittig, Staudinger, Appel and Corey-Fuchs reactions.1 I remember having a vial full of the white,
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
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.