Rh-Catalyzed Enantioselective Synthesis of 4-Substituted Heterocycles

Significance

Employing a tandem Rh-catalyzed C-H activation/Cope-rearrangement/elimination reaction, a variety of pyrrole vinyl acetates were converted into the corresponding 4-substituted indoles in moderate to excellent yields, and with excellent enantioselectivities. When R² and R³ formed a carbocycle, both the yields and enan­tioselectivities were excellent. This approach was extended to the synthesis of a 4-substituted benzothiophene and an interesting triindolyl compound.