University Paris-Sud 11, CNRS, BioCIS UMR 8076, Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, 5 rue J.-B. Clément, Châtenay-Malabry F-92296, France.
Org Lett. 2010 Sep 17;12(18):4042-5. doi: 10.1021/ol101639g.
PdCl(2)(MeCN)(2) in combination with dppp proved to be a powerful and efficient catalyst for the coupling of sterically hindered N-arylsulfonylhydrazones with aryl halides, thus providing a flexible and convergent access to tetrasubstituted olefins related to iso-combretastatin A4 in good yields. This new protocol has been applied successfully to the formal synthesis of biphenylisopropylidene 4-pyridine CYP17 inhibitor, 12b, of biological interest.
PdCl(2)(MeCN)(2)与 dppp 结合证明是一种强大而有效的催化剂，可用于将空间位阻的 N-芳基磺酰基腙与芳基卤化物偶联，从而以良好的收率提供了一种灵活和收敛的方法来合成与 iso-combretastatin A4 相关的四取代烯烃。该新方案已成功应用于具有生物活性的联苯异亚丙基 4-吡啶 CYP17 抑制剂 12b 的正式合成。
