Tang Ren-Jin, Milcent Thierry, Crousse Benoit
Faculty of Pharmacy, UMR 8076, BioCIS, Univ. Paris-Sud, CNRS, Université Paris-Saclay 92290 Châtenay-Malabry France
RSC Adv. 2018 Mar 13;8(19):10314-10317. doi: 10.1039/c8ra01397g.
An effective and clean FC alkylation of indoles and electron-rich arenes with β-nitroalkenes in HFIP was reported. The desired products are formed rapidly in excellent yields under mild conditions without the need for any additional catalysts or reagents. Further, this methodology can be applied to one-pot synthesis of biologically active tryptamine derivatives.
据报道,在六氟异丙醇(HFIP)中,吲哚和富电子芳烃与β-硝基烯烃发生了有效且清洁的傅-克烷基化反应。在温和条件下,无需任何额外的催化剂或试剂,就能迅速以优异的产率形成所需产物。此外,该方法可应用于生物活性色胺衍生物的一锅法合成。