J Org Chem. 2020 Feb 21;85(4):2697-2703. doi: 10.1021/acs.joc.9b02874. Epub 2020 Jan 10.
A regioselective halogenation of -benzyne derived from a nonaromatic enediyne core via Bergman cyclization and Suzuki-Miyaura coupling of the resulting haloarene in one-pot is disclosed. For the one-pot protocol to work, the reaction conditions were modified compared to an earlier reported procedure ( 2019 , 84 , 2911 - 2921 ) by reducing the amount of lithium iodide and exclusion of pivalic acid. Under these modified conditions, the products, benzo-fused tetrahydroisoquinoline-based biaryl derivatives were obtained in overall high to excellent yields (71-90%).
本文报道了一种通过 Bergman 环化和随后的卤代芳烃的 Suzuki-Miyaura 偶联反应，将源于非芳香型烯二炔核的 -苯炔进行区域选择性卤化的方法。为了实现一锅法反应，与早期报道的方法（2019 年，84，2911-2921）相比，本研究对反应条件进行了修改，减少了碘化锂的用量并排除了特戊酸。在这些改进的条件下，得到了苯并稠合四氢异喹啉基联芳基衍生物，总收率高至优秀（71-90%）。
