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 purification. The optimization was realized using the Design of Experiments approach and afforded a sustainable process suitable for industrial application.

中文翻译：

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2-丁基苯并呋喃的伸缩式混合间歇流合成


目前的工作描述了药物相关结构单元 2-丁基苯并呋喃 (BBF) 的改进合成方法的开发。伸缩式混合间歇流工艺由三个步骤组成，可提供高产率和纯度的最终产品。关键的环化步骤以连续模式进行，并进行集成后处理：与标准批量条件相比，这种方法更有效。产品的高质量使得BBF粗品无需纯化即可用于胺碘酮生产的下游工艺。使用实验设计方法实现了优化，并提供了适合工业应用的可持续工艺。