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MIYAURA BORYLATION

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!)

PROBLEMS WITH WASTE STREAMS

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

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