1,2-Disubstituted Bicyclo[2.1.1]hexanes as Bioisosteres of the ortho-substituted Benzene

1,2-Disubstitued bicyclo[2.1.1]hexanes have been designed, synthesized, and validated as a new generation of saturated bioisosteres of ortho-substituted benzenes. Incorporation of the bicyclo[2.1.1]hexane core into the structure of agrochemicals Boskalid (BASF), Bixafen (Bayer CS), and Fluxapyroxad (BASF) gave saturated analogs that exhibited a high antifungal activity.