Divergent Synthesis of Multisubstituted Hydroindole Derivatives via [3+2] Annulations of p‐Quinamines with Nitroalkenes

Abstract

The synthesis of two stereoisomers of hydroindole derivatives was achieved through [3+2] annulations of p‐quinamines with nitroalkenes. Catalyst‐free or in the presence of DMAP, the annulation reactions were employed to produce the target products containing four contiguous stereogenic centers. This method enables the efficient construction of multisubstituted and functionalized hydroindole derivatives from readily accessible building blocks and reagents. Furthermore, the anti‐inflammatory activity of some resulting hydroindoles was evaluated, with three derivative products showing effective inhibition of NLRP3 inflammasome activation.