Reactivity of N-protected 5-(2-bromophenyl)tetrazoles in palladium-catalyzed direct arylation of heteroarenes or fluorobenzenes

Add time:07/12/2019    Source:sciencedirect.com

A new route allowing the one-step synthesis of (2-heteroarylphenyl)tetrazole and fluorinated biphenyltetrazole derivatives is disclosed. By using 2 mol% of an air-stable diphosphine-palladium catalyst [PdCl(C3H5)(dppb)], potassium pivalate as base and dimethylacetamide as solvent, a wide range of heteroarenes (e.g., thiazoles, (benzo)thiophenes, furans, pyrroles, and imidazo[1,2-a]pyridine) and polyfluorobenzenes was easily coupled with N-protected (2-bromophenyl)tetrazoles in high yields.

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