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We have developed an efficient construction of 3-sulfonylindoles and 2-methyleneindophenols via decarboxylative propargylation/hydroamination of ethynyl benzoxazinanones using sodium sulfonates and phenols as the nucleophiles. The reaction featured mild conditions (K2CO3),… Click to show full abstract
We have developed an efficient construction of 3-sulfonylindoles and 2-methyleneindophenols via decarboxylative propargylation/hydroamination of ethynyl benzoxazinanones using sodium sulfonates and phenols as the nucleophiles. The reaction featured mild conditions (K2CO3), simple operation, and high chemoselectivity and was transition-metal-free. Our protocol could also be extended to other nucleophiles, including malonates, alcohols, and indoles. The broad substrate scope and scalability made this protocol practical for the synthesis of indole derivatives.
Journal Title: Organic letters
Year Published: 2021
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