2‐Oxabicyclo2.1.1hexanes: Synthesis, Properties, and Validation as Bioisosteres of ortho‐ and meta‐Benzenes

Abstract We have developed a general and practical approach towards 2‐oxabicyclo2.1.1hexanes with two and three exit vectors via an iodocyclization reaction. The obtained compounds have been easily converted into the corresponding building blocks for use in medicinal chemistry. 2‐Oxabicyclo2.1.1hexanes have been incorporated into the structure of five drugs and three agrochemicals, and validated biologically as bioisosteres of ortho ‐ and meta ‐benzenes.