abstract |
[PROBLEMS] To design a new method for producing 2,3-disubstituted indoles. [Solution] a) A bromoindole compound (i) is prepared with dialkoxyl C 1-5 borane in the presence of a ligand, a palladium catalyst and a base. Reacting to produce a compound of general formula (ii) or reacting compound (i) with a trialkylmagnesate reagent and then treating with borate; b) the product of step a is R2 Disclosed is a process for the preparation of 2,3 disubstituted indole compounds, such as compounds of general formula I, comprising the step of reacting with -Hal (R2-Hal is defined herein). [Selection figure] None |