This invention provides a one-
step method for preparing 4-substituted indole. Using 2-methyl-3-
nitroaniline as a
raw material,
acetic anhydride is slowly added after dissolving it in DMF
solvent with low-temperature stirring. After the
condensation reaction is completed, DMF-DMA and tetrahydropyrrole are directly added. A cyclization reaction is carried out in stages with controlled temperature, and
methanol byproducts are evaporated. After cooling the reaction solution,
ice water is added dropwise to crystallize and obtain a crude product. This crude product is then dissolved in 2-methyltetrahydrofuran, washed with
hydrochloric acid, washed with water, washed with a saturated
sodium bicarbonate aqueous solution, decolorized with
activated carbon, concentrated, and recrystallized with
acetonitrile to obtain high-purity 4-substituted indole. This invention employs a one-step
continuous reaction, eliminating multiple purification steps such as intermediate separation, washing, and
drying, significantly simplifying the process and shortening the
production cycle. Compared with traditional processes, the yield is significantly improved, with fewer byproducts, lower
energy consumption, and smaller emissions. The process is stable, reliable, simple, and safe to operate, suitable for industrial production, and meets the requirements of high-end pharmaceutical intermediates.