Cycloisomerization/cyclization cascade reactions for yne-enones and enyamides can be used to construct diverse fused furans, however, the corresponding (2 + n) reaction remains challenging. Here, the authors report cycloisomerization/(2 + 3) cycloadditions catalyzed by silver acetate and a modified chiral pyrrolidinopyridine relay system, to generate bispirocyclopentene pyrazolone products with isoform-selective phosphodiesterase 1 (PDE1) inhibitory activity.
