Water-compatible acylation reactions with acid chlorides using a flow microreactor

Abstract

In this study, we used a flow microreactor for acylation with acid chlorides in a homogeneous aqueous medium, suppressing hydrolysis and providing up to 98% yield. Quenched-flow analysis indicated an associative transition state. This method applies to amines, phenols, thiols, and pharmaceuticals. Acylation of oseltamivir proceeds with a throughput of 2.1 g h⁻¹, demonstrating scalability and practicality.