摘要 : Bioisosteres play an important role in pharmaceutical and agricultural compound design that has been developed to enhance the properties of molecules.As a sp3-rich small ring cage hydrocarbons,bicyclo[1.1.1]pentanes(BCPs)were comm... 展开 Bioisosteres play an important role in pharmaceutical and agricultural compound design that has been developed to enhance the properties of molecules.As a sp3-rich small ring cage hydrocarbons,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 improve pharmacokinetic properties,including passive permeability,aqueous solubility,metabolic stability[1].Over the past decades,numerous pharmaceutically relevant molecules with biaryl frameworks were improved by the approach of bioisosteric replacement.Conventional strategies for the synthesis of such BCP-aryls derivatives mostly depend on the stepwise C-C formation via the direct addition to bridgehead C-C bond of[1.1.1]propellane to provide active BCP-intermediates and followed by a second transitionmetal cross-coupling sequence.However,these pioneer works were limited by the low step economy,the use of unstable reagents,and harsh conditions in industrial productions. 收起