The Buchwald-Hartwig coupling enables the grafting of nitrogen-containing functionalities onto molecules,facilitating the synthesis of a wide variety of molecular structures.However,several challenges impact the susta...The Buchwald-Hartwig coupling enables the grafting of nitrogen-containing functionalities onto molecules,facilitating the synthesis of a wide variety of molecular structures.However,several challenges impact the sustainability of this coupling.In our pursuit of a more sustainable Buchwald-Hartwig process,we report an optimized protocol that enhances energy efficiency and minimizes waste.Utilizing recoverable Pd/C as a catalyst,we performed the process in the bio-based solvent 2-MeTHF.To further boost energy efficiency,we employed microwave heating technology,resulting in improved overall process efficiency and reduced reaction times.This optimized approach allowed for the synthesis of a wide array of 17 variously functionalized arylamines.Thanks to the optimized workup procedure that facilitated the recovery and reuse of the catalyst,ligand,and 2-MeTHF,we achieved a reduced E-Factor ranging from 5.8 to 14.9,further contributing to the sustainability of the process.展开更多
基金funding by the European Union–NextGenerationEU under the Italian Ministry of University and Research(MUR)National Innovation Ecosystem grant ECS00000041–VITALITY.
文摘The Buchwald-Hartwig coupling enables the grafting of nitrogen-containing functionalities onto molecules,facilitating the synthesis of a wide variety of molecular structures.However,several challenges impact the sustainability of this coupling.In our pursuit of a more sustainable Buchwald-Hartwig process,we report an optimized protocol that enhances energy efficiency and minimizes waste.Utilizing recoverable Pd/C as a catalyst,we performed the process in the bio-based solvent 2-MeTHF.To further boost energy efficiency,we employed microwave heating technology,resulting in improved overall process efficiency and reduced reaction times.This optimized approach allowed for the synthesis of a wide array of 17 variously functionalized arylamines.Thanks to the optimized workup procedure that facilitated the recovery and reuse of the catalyst,ligand,and 2-MeTHF,we achieved a reduced E-Factor ranging from 5.8 to 14.9,further contributing to the sustainability of the process.