Access to Piperazine-Fused Pyrrolocarbazoles Enabled\nby Acid-Catalyzed Stereoselective Hydroarylation of Ynamide–Indoles\nand Subsequent Diels–Alder Reactions/Aromatizations

Pyrrolocarbazole\nskeletons are well known to possess a variety\nof biological activities that might be therapeutically useful in the\ntreatment of cancers. Herein, an acid-catalyzed stereoselective hydroarylation/Diels–Alder\ncycloaddition/aromatization of ynamide–indoles is described.\nWe newly designed and synthesized a variety of piperazine-fused pyrrolocarbazole\nderivatives that could be further applied to the synthesis of potent\nWee1 inhibitors.