Institut für Biochemie, Ernst-Moritz-Arndt-Universität Greifswald , Felix-Hausdorff-Str. 4, 17489 Greifswald, Germany.
Department of Chemistry, Institute of Chemical Technology , Nathalal Road, Matunga, Mumbai 400019, India.
Org Lett. 2018 Jan 19;20(2):473-476. doi: 10.1021/acs.orglett.7b03854. Epub 2018 Jan 5.
A mild and highly efficient catalytic amination procedure for chloroheteroarenes at ambient temperature using the Pd/PTABS catalytic system is reported. The protocol is selective for the amination of chloroheteroarenes using secondary amines such as piperidine, pyrrolidine, and several others. The exceptional mildness of the developed protocol is beneficial for the synthesis of a crucial Buparlisib intermediate as well as the formal synthesis of Alogliptin in competitive yields.
报道了一种温和、高效的室温下钯/PTABS 催化体系催化氯代杂芳烃的氨化反应。该方法对仲胺如哌啶、吡咯烷等的氯代杂芳烃的氨化反应具有选择性。所开发的温和条件对关键中间体 Buparlisib 的合成以及阿格列汀的形式合成具有重要意义，并且能够以竞争性收率得到目标产物。
