Dai Xi-Jie, Engl Oliver D, León Thierry, Buchwald Stephen L
Department of Chemistry, Room 18-490, Massachusetts Institute of Technology, Cambridge, MA, 02139, USA.
Angew Chem Int Ed Engl. 2019 Mar 11;58(11):3407-3411. doi: 10.1002/anie.201814331. Epub 2019 Feb 15.
Herein, we report a practical two-step synthetic route to α-arylpyrrolidines through Suzuki-Miyaura cross-coupling and enantioselective copper-catalyzed intramolecular hydroamination reactions. The excellent stereoselectivity and broad scope for the transformation of substrates with pharmaceutically relevant heteroarenes render this method a practical and versatile approach for pyrrolidine synthesis. Additionally, this intramolecular hydroamination strategy facilitates the asymmetric synthesis of tetrahydroisoquinolines and medium-ring dibenzo-fused nitrogen heterocycles.
在此，我们报道了一种通过铃木-宫浦交叉偶联反应和对映选择性铜催化分子内氢胺化反应合成α-芳基吡咯烷的实用两步合成路线。该反应具有出色的立体选择性，并且对于含有药学相关杂芳烃的底物转化具有广泛的适用范围，这使得该方法成为一种实用且通用的吡咯烷合成方法。此外，这种分子内氢胺化策略有助于四氢异喹啉和中环二苯并稠合氮杂环的不对称合成。
