Water → 1H-Indole, 3-(5-bromo-2-chloro-4-pyrimidinyl)-1-[(4-methylphenyl)sulfonyl]-

Participants

Reaction Conditions

Reaction Steps

3-(5-Bromo-2-chloropyrimidin-4-yl)-1H-indole (INTERMEDIATE 5, 1.23 g, 4 mmol) in THF (40.0 ml) and DMF (5 ml) was cooled to −10° C. Sodium hydride (0.19 g, 4.80 mmol) was added and the reaction was stirred at −10° C. for 30 min. 4-Methylbenzene-1-sulfonyl chloride (0.84 g, 4.40 mmol) was then added. The reaction mixture was allowed to warm to RT and stirred for 15 h. Water (10 mL) was added and the resultant solids were collected by vacuum filtration to give the title product (1.36 g, 73.5%).

Provenance & Evidence