Synthesis of Three-Dimensional Ring Fused Heterocycles by a Selective [4+2] Cycloaddition Between Bicyclic Thiazolo 2-Pyridones and Arynes

A selective [4 + 2] cycloaddition reaction of thiazolo-2-pyridones with arynes has been demonstrated. The developed protocol allows rapid access to highly functionalized, structurally complex thiazolo-fused bridged isoquinolones in high yields, which are susceptible to further late-stage functionalization.