Multi Kilogram-Scale Synthesis of an Anticancer Drug Candidate: A Journey Towards Development of Some Key Reactions

in order to evaluate a new drug in preclinical or clinical testing, the pharmaceutical industry needs bulk quantities of final product (from kg to hundreds of kg). Converting reactions from laboratory into industrial-scale manufacturing processes remains a challenge for process chemists while taking into account safety, legislation, environmental and cost of goods requirements.

As part of a drug discovery program at Servier Group, compound 1 was selected. To enable further clinical studies, we explored an efficient route to synthesize 1 implementing some key reactions.

Both strategy and scale up will be discussed.