Multiple C–H Activation Enabled Modular Construction of Densely Functionalized Sulfur-Contained Arenes

21 January 2021, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


Modular construction of multiple functionalized arenes from abundant feedstocks, stands as an unremitting pursue goal in synthetic chemistry, which would accelerate the discovery of new drugs an advanced materials. Herein, by using multiple C-H activation strategy, through judicious choice of versatile imidate ester as the key directing group, expedi-ent delivery of molecular libraries of densely functionalized sulfur-contained arenes. Further synthetic application was demonstrated by multiple C-H modification of fused arenes and pharmaceuticals such as Ibuprofen, and concise con-struction of biologically active molecules, Madam dihydrochloride and Bipenamol, was also achieved.


Multiple C-H activation
Tunable selectivity
Densely functionalized arenes
Multiple Cross-Dehydrogenative Coupling
Rhodium CatalysisA


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