In the decades after the discovery of the Conia-ene reaction, several improvements allowed for milder reaction conditions and greater control of product stereo- and regiochemistry. For example, the carbonyl component, formerly a ketone or aldehyde, became a substituted β-ketoester or malonate ester. Such carbonyls enolize much more readily, yielding better access to the desired enol tautomer. Additionally, the alkene component was replaced with an alkyne, which not only gave better cyclization in accordance with Baldwin’s rules, but also furnished a product containing an alkene that served as a useful handle for further transformations. Finally, recent efforts have featured metal-mediated and metal-catalyzed Conia-ene reactions that can be rendered asymmetric using chiral ligands.