Dengue virus is a worldwide health threat with 400 million yearly infections. Given a lack in specific therapeutics, the current work reports DENV2 inhibitory activity in newly designed compounds that are more potent than the standard drug ribavirin.
We report the first examples of scandium-catalyzed spirocyclization between simple BCBs and azomethine imines, establishing a new platform for the synthesis of previously inaccessible 6,7-diazaspiro[3.4]octanes.
Developments in the synthesis and application of strained spiro heterocycles are discussed, given their potential as non-classical rigid three-dimensional bioisosteres in drug development.
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.
An efficient bromo-lactamization mediated neighboring group participation approach for synthesizing a novel 3D framework, spiro-isoxazoline-lactam, was developed.