1014613-05-8

1014613-64-9

General procedure for the synthesis of 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine from 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine: To 4-bromo-2-methyl-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine (16 g, 0.045 mol) of 1,4-dioxane ( 320 mL) solution was added to 2M aqueous sodium hydroxide solution (114 mL, 0.228 mol). The reaction mixture was heated to 60°C and kept for 16 hours. After the reaction was completed, the mixture was cooled to room temperature. The organic layer was separated and the aqueous layer was extracted with ethyl acetate. The organic phases were combined, washed with saturated brine, dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure to give 4-bromo-2-methyl-1H-pyrrolo[2,3-b]pyridine as a milky white solid (10.07 g, 104% yield). lC/MS (Method B): m/z 211/213 [M+H]+, retention time 1.04 min.