One‐Pot Two‐Step Synthesis of Isochromene‐Fused CF3‐Substituted Pyrazoles

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An efficient one‐pot, two step method for fusing two biologically active motifs, CF3‐substituted pyrazoles and isochromenes, was developed. Selective O‐benzylation of CF3‐substituted pyrazolones and subsequent Pd‐catalyzed direct C–H arylation generate a fused tricycle. For the synthesized compounds through‐space 13C–19F spin–spin coupling was revealed. In addition, the synthesis of three thioisochromene analogues, and one isocoumarin derivative, was accomplished.