Porte Vincent, Kollmus Philipp, Serrano Eloisa, Santagostino Marco
Chemical Development Germany, Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach an der Riß, 88397, Germany.
Chemistry. 2025 Feb 20;31(11):e202403795. doi: 10.1002/chem.202403795. Epub 2025 Jan 21.
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.
报道了一种新型筛选平台,用于在低负载量下利用空气稳定的Ni(COD)DQ实现(杂)芳基卤化物的镍催化氰化反应。通过高通量实验(HTE),系统地探索了各种配体和溶剂组合,从而能够快速确定合适的条件。这种标准化的工作流程是选择其他有效镍预催化剂以及进一步优化难反应底物的良好起点。该转化反应具有广泛的官能团耐受性,并且可以很容易地放大至克级规模。