A novel diastereoselective one-pot protocol has been developed through sequential execution of an aza-Piancatelli rearrangement and a Conia-ene type reaction under Lewis acid catalysis.
Highly efficient synthesis of diverse 2,2-disubstituted 3-methyleneindoline derivatives through a one-pot base-promoted post-Ugi 5-exo-dig “Conia-ene”-type cyclization has been disclosed.
We disclose a gold-catalyzed conversion of unactivated β-ketopropargyl amines to polysubstituted pyrroles under mild, operationally simple conditions. This protocol was further extended to synthesize indolizine skeleton via a one-pot process.
A two-step Kinugasa/Conia-ene-type sequential reaction is developed. The process provided a simple and efficient access to chiral 8-methylene-2,6-diazaspiro[3.4]octane-1,5-diones.
A metal-free protocol utilizing DBU catalysis for post-Ugi amide-ester exchange and Conia-ene double cyclization has been successfully developed, allowing the synthesis of diverse highly functionalized benzo-fused spiroindolines with anti-cancer activities under mild conditions.