62606-00-2

3-Bromo-5-(methylsulfonyl)aniline is used in the preparation of WDR5-?MYC inhibitors.

General procedure for the synthesis of 3-bromo-5-(methylsulfonyl)aniline from 1-bromo-3-(methylsulfonyl)-5-nitrobenzene: 1-bromo-3-(methylsulfonyl)-5-nitrobenzene (100 mg, 0.4 mmol) was dissolved in tetrahydrofuran (THF, 10 mL). Raney nickel catalyst was added and the hydrogenation reaction was carried out under 1 bar hydrogen pressure. Upon completion of the reaction, the mixture was filtered to remove the catalyst and the filtrate was subsequently concentrated. 3-Bromo-5-(methylsulfonyl)aniline (30 mg, 0.16 mmol, 40% yield) was finally obtained as a yellow solid.

[1] Patent: EP1953163, 2008, A1. Location in patent: Page/Page column 13
[2] Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999), 1977, p. 14 - 17