Cambrex Profarmaco Milano Srl

The present work describes the development of an improved synthesis of the pharmaceutically relevant building block 2-butylbenzofuran (BBF).The telescoped hybrid batch-flow process is composed of three steps and affords the final product in high yield and purity.The key cyclization step is performed in continuous mode with integrated workup: this approach is more efficient compared to the standard batch conditions.The high quality of the product makes crude BBF suitable to be used in the downstream process of production of amiodarone without purificationThe optimization was realized using the Design of Experiments approach and afforded a sustainable process suitable for industrial application.

Safety of the patient must be considered as the reference point for the producers of compounds for the pharmaceutical market.In this paper, starting from the case study of Brexpiprazole, we describe the essential aspects connected to the development of sustainable processes for the production of Active Pharmaceutical Ingredients (APIs).