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A rhodium‐catalyzed methodology leads to four kinds of novel podophyllotoxin derivatives starting from readily available podophyllotoxin in a late‐stage functionalization strategy. Some of them are found to show excellent anticancer activity. This direct C−H functionalization can be expressed the podophyllotoxin (roots of podophyllum species) being converted into derivatives (leaves) by rhodium catalysis...
A divergent synthesis of podophyllotoxin derivatives from simple and readily available starting materials through a late‐stage functionalization strategy by rhodium catalysis is reported here. This strategy uses the ketone and oxime in substrates as directing groups. Four kinds of novel podophyllotoxin derivatives have been obtained without any erosion of the enantiopurity, thus indicating the broad...