Bioisosteric replacement of benzenes with caged hydrocarbons can form enhanced lead compounds with improved drug-like properties, but synthetic challenges limit their application. Now, a collective strategy for synthesizing saturated bioisosteres of 1,2,4-trisubstituted and disubstituted benzenes has been developed. This strategy involves constructing 2-thiabicyclo[3.1.1]heptane scaffolds via cycloaddition of bicyclo[1.1.0]butanes and mercaptoacetaldehyde.
- Feng Wu
- Ji-Jie Wang
- Jian-Jun Feng
