The application relates to the technical field of
chemical synthesis, and particularly discloses a synthesis method of a triplet
carbene-mediated C2-substituted bicyclo[1.1.1]
pentane derivative, which successfully opens up a synthesis path of C2-substituted bicyclo[1.1.1]
pentane (BCP) by inserting bicyclo[1.1.0]
butane (BCB) under photosensitive conditions; the 1,4-dibasic radical species generated by the triplet
carbene has a faster
recombination rate; the method not only lays a
solid foundation for the application of bicyclo[1.1.1]
pentane in
medicinal chemistry, but also overcomes the limitation of traditional
benzene rings in
metabolic stability and water
solubility by replacing a
bioisostere and using a three-dimensional bridged ring structure. In addition, the synthesized derivatives exhibit excellent
biological activity, and experimental data prove that the derivatives have significant fungal inhibition activity in tests such as
botrytis cinerea, thereby providing important
technical support for the design and development of new drugs.