Access to 2‑Oxabicyclo[2.1.1]hexanes\nand their\nuse in Scaffold Hopping

Saturated isosteres of the <i>ortho</i>-substituted\nbenzene\nring remain rare due to the paucity of methods to access complex bridged\nsystems. Using blue-light-mediated [2 + 2] photocycloaddition chemistry,\nwe have developed a quick and practical route to provide novel 2-oxabicyclo[2.1.1]hexanes\nfrom simple feedstock materials in only three steps. Matched pair\nanalysis confirmed that this motif could prove useful in the future\nto the drug discovery community as a scaffold endowed with remarkable\nproperties.