The Lab Notes

Louis Diorazio and co-workers at AstraZeneca recently published an article entitled “Toward a More Holistic Framework for Solvent Selection”, which describes the development of a solvent selection tool. Most solvent guides concentrate on Health and Environmental aspects of solvents, but where this new solvent selection tool differs is that it takes in to account issues…

At the recent 'Scale Up of Chemical Processes Conference' in Baveno, Italy, John Snoonian of Sunovion discussed the development and scale up of a manufacturing route to make a 5HT4 partial agonist containing a 1,2,4-oxadiazole ring. During route scouting studies on the synthesis of the benzopyrazole an interesting solvent effect was observed – see Scheme…

At the recent 'Scale Up of Chemical Processes Conference' in Baveno, Italy, Charles Papageorgiu of Eisai described the optimization of a borylation process to prepare boronic acid ML-826 (see Scheme 1). Scheme 1: Preparation of boronic acid ML-826 The original method using B2Pin2 and Pd(PPh3)2Cl2 as catalyst was extremely inefficient (9.25 day batch cycle time!)…

At the recent 'Scale Up of Chemical Processes Conference' in Baveno, Italy, Wim Dermaut from Agfa presented some case studies where problems have occurred as a result of reactive chemicals present in waste streams. In the first case study a drum containing a waste stream including diethylhydroxylamine exploded. The most likely cause was caustic present…