Use of a “Catalytic” Cosolvent,N,N‐Dimethyl Octanamide,Allows the Flow Synthesis of Imatinib with no Solvent Switch |
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Authors: | Jeffrey C. Yang Dawen Niu Bram P. Karsten Fabio Lima Stephen L. Buchwald |
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Abstract: | A general, efficient method for C−N cross‐coupling has been developed using N,N‐dimethyloctanamide as a catalytic cosolvent for biphasic continuous‐flow applications. The described method was used to generate a variety of biarylamines and was integrated into a two‐step sequence which converted phenols into biarylamines via either triflates or tosylates. Additionally, the method was applied to a three‐step synthesis of imatinib, the API of Gleevec, in good yield without the need of solvent switches. |
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Keywords: | Biaryle Durchflusschemie Kreuzkupplungen Palladium Synthesemethoden |
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