铑催化动力学拆分实现立体选择性多取代双环[1.1.0]丁烷合成

Xiaolong Zhang1†, Rongkai Wu2†, Zhaohong Liu1*, Ge Yin1, Jiaqi Tang1, Paramasivam Sivaguru1, Xin Hong2,3*, Edward A. Anderson4, Xihe Bi1,5,6* bicyclo[1.1.0]butanes (bcbs) are a distinctive class of strained small-ring carbocycles of growing importance in synthetic and medicinal chemistry. However, the enantioselective synthesis of polysubstituted bcbs remains a largely unsolved challenge. In this study, we report a general chemical platform for the stereoselective assembly of chiral or meso 1,2,3,4-tetrasubstituted bcbs from internal alkynes and carbenes through stepwise [2+1+1’] or one-pot [2+1+1] cycloaddition reactions, respectively. Successful execution of these transformations exploits the combination of triftosylhydrazones (carbene precursors) and chiral dirhodium catalysts. …