Post-Ugi modifications offer a great tool to construct functionalized heterocycles in an atom-economic manner. Using this approach, we have constructed highly functionalized azaspiro tricyclic scaffolds that involve Ugi condensation and ipso-cyclization followed by aza-Michael ring closures. Herein, we present a detailed account of aza-Michael cyclizations with respect to substrate scope and limitations, along with new methods to prepare novel azaspiro tricyclic scaffolds.

The Cover Feature depicts a gradual process for synthesizing complex azaspiro tricyclic scaffolds starting from common building blocks through substrate‐selective post‐Ugi modifications that involve spirocyclization and aza‐Michael addition, which is depicted by analogy with a tree. The starting materials are illustrated as the soil nutrients that are taken up by roots to generate Ugi adducts. The cover picture was designed by Mr. Kazim, Mr. Mayur D. Ambule, Mr. Mandweep Bhumij, and Dr. Ajay Kumar Srivastava. More information can be found in the Research Article by A. Kumar Srivastava et al.