3-CHLORO-6-BROMO INDOLE synthesis

Yield:57916-08-2 94%

Reaction Conditions:

with 1,3-Dichloro-5,5-dimethyl-2,4-imidazolidinedione in 1,4-dioxane at 25; for 3 h;

Steps:

General Procedure for the 3-chlorination of Indoles

General procedure: DCDMH(108mg, 0.55mmol) was added to a solution of indoles (1.0 mmol) in 1.4-dioxaneat room temperature, and the resulting solution was stirred up to transformcompletely. The reaction solution was poured into the saturated NaHCO₃solution (10 mL), the mixtures was extracted by ethyl acetate (15 ml*2). The organic phase was dried over Na₂SO₄,filtered, concentrated under reduced pressure. The residue was then purified byflash chromatography on 200~300 mesh silica gel to provide the correspondingproduct 4.

References:

Yan, Jianwei;Ni, Tianjun;Yan, Fulin [Tetrahedron Letters,2015,vol. 56,# 9,p. 1096 - 1098] Location in patent:supporting information