posted on 2024-02-29, 15:05authored byLin-Lin Ma, You Zhou, Yong-Xing Tang, Ting Chen, Zheng-Hao Wang, Yan-Dong Wu, Jun-Gang Wang, An-Xin Wu
An efficient synthetic method for
constructing 2,3- and
2,4-disubstituted
pyrimidio[1,2-b]indazole skeletons through I2-DMSO-mediated and substrate-controlled regioselective [4
+ 2] cyclization is reported. The reaction conditions are mild, its
operation is simple, and the substrate scope is wide. More than 60
pyrimidio[1,2-b]indazole derivatives have been synthesized,
providing a new methodology for constructing related molecules and
potentially enriching bioactive-molecule libraries.