Preparation of 2-(2H-Tetrazol-2-yl)benzoic Acids via Regioselective Cu(I) Catalyzed N2 Arylation of Tetrazole,Organic Process Research & Development

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Preparation of 2-(2H-Tetrazol-2-yl)benzoic Acids via Regioselective Cu(I) Catalyzed N2 Arylation of Tetrazole
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-10-14 , DOI: 10.1021/acs.oprd.9b00243
Zhiguo Jake Song ₁ , Peter Maligres ₁ , Carmela Molinaro ₁ , Guy Humphrey ₁ , Jeff Fritzen ₁ , Jonathan Wilson ₁ , Yonggang Chen ₁

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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.

中文翻译：

区域选择性Cu（I）催化四唑的N2芳基化反应制备2-（2 H-替他唑-2-基）苯甲酸

2-（2 H-替他唑-2-基）苯甲酸1及其类似物是通过Cu（I）催化2-碘或2-溴苯甲酸与5-（乙硫基）-1 H-四唑的C–N偶联制备的然后还原性裂解硫醚键。C–N偶联对四唑的N2-位置具有区域选择性。在一系列2-卤代苯甲酸底物上以中等收率证明了该方法的范围。

更新日期：2019-10-14

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