反应详情

To a solution of commercially available 6-chloro-3-formyl-1H-indole-2-carboxylic acid ethyl ester in t-BuOH and 2-methyl-2-butene (50 eq) was added 9.2 eq NaClO2 (9 eq) and aq. NaH2PO4 (7 eq) and stirred 12 h at room temperature. After concentration the mixture was dissolved in H2O and adjusted to pH7 and then extracted with EtOAc; partial concentration of the organic phase precipitated the product in 52% yield.

1. concentrationAfter concentration the mixture
2. dissolutionwas dissolved in H2O
3. extractionextracted with EtOAc
4. concentrationpartial concentration of the organic phase
5. customprecipitated the product in 52% yield