Continuous‐/Micro‐Flow Reactions Using Highly Electrophilic PCl₃ and POCl₃

Abstract

Figure 1. a) Chemical structure of phosphorus-containing compounds. b) Chemical structure of representative phosphorylating reagents.

Rapid production of the anaesthetic mepivacaine through continuous, portable technology

“…By taking advantage of a flow setup, they successfully used the same heterogeneous catalyst (10% Pd/C) and reducing agent (H 2(g) ) for both reactions, overcoming reagent toxicity and improving process safety. Nevertheless, this strategy still has some drawbacks such as the requirement of hydrogen (or hydrogen generators in situ such as an H-cube), generation of HCl (g) upon amide coupling and the need to use PCl 3 as a chlorinating reagent, leading to the formation of large amounts of phosphorus-derived waste that is difficult to process, 19 lowering in this way the atom economy and greenness of the overall synthesis. In addition, the transposition to flow of the first step was not attempted due to the formation of precipitates that could lead to reactor clogging.…”