Department of Chemistry , Zhejiang Sci-Tech University , Xiasha Campus, Hangzhou 310018 , People's Republic of China.
Leibniz-Institut für Katalyse e. V. an der Universität Rostock , Albert-Einstein-Straβe 29a , 18059 Rostock , Germany.
Org Lett. 2019 Jul 19;21(14):5694-5698. doi: 10.1021/acs.orglett.9b02037. Epub 2019 Jun 27.
A cobalt-catalyzed C-H carbonylation of naphthylamides for the synthesis of benzo[]indol-2(1)-one scaffolds has been developed. The reaction employs a traceless directing group and uses benzene-1,3,5-triyl triormate as the CO source, affording various free ()-benzo[]indol-2(1)-ones in moderate to high yields (up to 88%). Using this protocol, the total synthesis of BET bromodomain inhibitors A and B was accomplished as well.
发展了一种钴催化的萘甲酰胺 C-H 羰基化反应，用于合成苯并[]吲哚-2(1)-酮骨架。该反应采用无痕迹导向基团，使用苯-1,3,5-三羧酸三甲酯作为 CO 源，以中等至较高的收率（高达 88%）得到各种游离的（）-苯并[]吲哚-2(1)-酮。利用该方案，还完成了 BET 溴结构域抑制剂 A 和 B 的全合成。
