Mild Base-Promoted Tandem Nucleophilic Substitution/ Decarboxylation/Hydroamination: Access to 3-Sulfonylindoles and 2-Methyleneindophenols
ORGANIC LETTERS(2021)
摘要
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.
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关键词
tandem nucleophilic substitution/decarboxylation/hydroamination,base-promoted
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