High-throughput Experimentation Enables the Development of a Nickel-catalyzed Cyanation Platform for (Hetero)aryl
Vincent Porte1, Philipp Kollmus1, Eloisa Serrano1
1Chemical Development Germany, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach an der Riß, 88397, Germany.
Abstract:
A novel screening platform for the nickel-catalyzed cyanation of (hetero)aryl halides relying on the use of air-stable Ni(COD)DQ at low loading is reported. Through high-throughput experimentation (HTE), various ligand and solvent combinations are systematically explored, allowing the fast identification of suitable conditions. This standardized workflow serves as an excellent starting point for selecting other competent nickel precatalysts and for further optimization of reluctant substrates. The transformation exhibits broad functional group tolerance and can be readily scaled up to gram-scale.
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