Catalyst‐Switchable Regiocontrol in the Direct Arylation of Remote CH Groups in Pyrazolo[1,5‐a]pyrimidines |
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| Authors: | ProfDr Robin B Bedford Dr Steven J Durrant Michelle Montgomery |
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| Institution: | 1. School of Chemistry, University of Bristol, Cantock's Close, Bristol, BS8 1TS (UK);2. Vertex Pharmaceuticals Ltd. (Europe), 86‐88 Jubilee Avenue, Milton Park, Abingdon, Oxfordshire, OX14 4RW (UK) |
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| Abstract: | The regiodivergent palladium‐catalyzed C? H arylation of pyrazolo1,5‐a]pyrimidine has been achieved, wherein the switch in regioselectivity between positions C3 and C7 is under complete catalyst control. A phosphine‐containing palladium catalyst promotes the direct arylation at the most acidic position (C7), whereas a phosphine‐free catalyst targets the most electron‐rich position (C3). |
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| Keywords: | arylation catalysis C H activation palladium regiocontrol |
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