Zhang Yitao, Takale Balaram S, Gallou Fabrice, Reilly John, Lipshutz Bruce H
Department of Chemistry and Biochemistry , University of California Santa Barbara , Santa Barbara , CA 93106 , USA . Email:
Novartis Pharma AG , Basel , Switzerland.
Chem Sci. 2019 Sep 20;10(45):10556-10561. doi: 10.1039/c9sc03710a. eCollection 2019 Dec 7.
A 1 : 1 Pd : ligand complex, [-BuXPhos(Pd-π-cinnamyl)]OTf, has been identified as a highly robust pre-catalyst for amination reactions leading to diarylamines, where loadings of metal are typically at 1000 ppm Pd, run in water at temperatures between rt and 45 °C. The protocol is exceptionally simple, is readily scaled, and compares very favorably traditional amination conditions. It has also been shown to successfully lead to key intermediates associated with several physiologically active compounds.
一种1:1的钯：配体络合物，即[-叔丁基XPhos（钯-π-肉桂基）]三氟甲磺酸盐，已被确定为用于生成二芳基胺的胺化反应的一种高度稳定的预催化剂，其中金属负载量通常为1000 ppm钯，该反应在水相中于室温至45°C的温度下进行。该方案异常简单，易于放大，与传统胺化条件相比具有很大优势。它还已被证明能成功生成与几种生理活性化合物相关的关键中间体。
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