Double carbonylation of iodobenzene in a microfluidics-based high throughput flow reactor

Double carbonylation of iodobenzene in the presence of amines were carried out effectively in a microfluidics-based flow reactor (X-Cube™) of high throughput capability using immobilized Pd(PPh3)4 catalyst. By the proper tuning of the reaction conditions α-ketoamides could be synthesized with 70–96% selectivities depending on the choice of the nucleophile. The highest yields of double carbonylation products were obtained at relatively low temperature (80 °C) and using DBU as the base with primary amines as the reaction partners. Imine formation was observed only at higher temperatures.

Graphical abstractDouble carbonylation of iodobenzene in the presence of amines were carried out effectively in a microfluidics-based flow reactor (X-Cube™) of high throughput capability using immobilized Pd(PPh3)4 catalyst. By the proper tuning of the reaction conditions α-ketoamides could be synthesized with 70–96% selectivities depending on the choice of the nucleophile. The highest yields of double carbonylation products were obtained at relatively low temperature (80 °C) and using DBU as the base with primary amines as the reaction partners. Imine formation was observed only at higher temperatures.Figure optionsDownload full-size imageDownload as PowerPoint slide