Preparation of 2‑(2H‑Tetrazol-2-yl)benzoic Acids via Regioselective Cu(I) Catalyzed N2 Arylation of Tetrazole

Organic Process Research & Development(2019)

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摘要
2-(2H-Tetrazol-2-yl)­benzoic acid 1 and analogs were prepared via Cu­(I) catalyzed C–N coupling of 2-iodo or 2-bromo benzoic acids with 5-(ethylthio)-1H-tetrazole followed by reductive cleavage of the thioether bond. The C–N coupling was regioselective toward the N2-position on tetrazole. The scope of this methodology was demonstrated on a series of 2-halobenzoic acid substrates in moderate yields.
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关键词
Tetrazole benzoic acid,N-2 regioselective tetrazole arylation
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