Zhou Ze, Huang Xiang, Wei Qing-Yi, Wang Yi-Lin, Wu Bin, Yang Jin-Ming
School of Pharmaceutical Sciences, South-Central Minzu University, Wuhan 430074, People's Republic of China.
Org Lett. 2024 Sep 6;26(35):7273-7278. doi: 10.1021/acs.orglett.4c01889. Epub 2024 Aug 12.
Pyrrolocarbazole skeletons are well known to possess a variety of biological activities that might be therapeutically useful in the treatment of cancers. Herein, an acid-catalyzed stereoselective hydroarylation/Diels-Alder cycloaddition/aromatization of ynamide-indoles is described. We newly designed and synthesized a variety of piperazine-fused pyrrolocarbazole derivatives that could be further applied to the synthesis of potent Wee1 inhibitors.
众所周知，吡咯并咔唑骨架具有多种生物活性，这些活性在癌症治疗中可能具有治疗用途。在此，描述了一种酸催化的烯酰胺吲哚的立体选择性氢芳基化/狄尔斯-阿尔德环加成/芳构化反应。我们新设计并合成了多种哌嗪稠合的吡咯并咔唑衍生物，这些衍生物可进一步应用于高效Wee1抑制剂的合成。
