Bioisosteres play an important role in pharmaceutical and agri cultural compound design that has been developed to enhance the properties of molecules.As a sp3-rich small ring cage hydro carbons,bicyclo[1.1.1]pentanes （BCPs） were commonly considered as a bioisostere of the para-substituted arenes,internal alkynes and tert–butyl groups,and its introduction can significantly im prove pharmacokinetic properties,including passive permeability aqueous solubility,metabolic stability[1].Over the past decades numerous pharmaceutically relevant molec...
