Design, synthesis and biological evaluation of difluoroalkylated protoilludanes obtained by a practical radical cascade difluoroalkylation-cyclization reaction

• Difluoroethylation-cyclization of b-Caryophyllene with iododifluoromethyl ketones. • Synthesis difluoroalkylated protoilludanes by one step. • These fluorinated compounds displayed interesting biological activities against human ovarian cancer cells (A2780 and SKOV-3) and lung cancer cells (A549). A radical cascade difluoroalkylation-cyclization of β-Caryophyllene with iododifluoromethyl ketones provides a practical method for the synthesis of difluoroalkylated protoilludanes in excellent yield. Further, these fluorinated compounds displayed interesting biological activities against human ovarian cancer cells (A2780 and SKOV-3) and lung cancer cells (A549) showcasing the value of this modification strategy.