反应详情

To a solution of 1-(4-(4-((cyclobutylamino)methyl)-3-fluorophenyl)piperazin-1-yl)ethanone (55 mg, 0.18 mmol) in dichloromethane (1 mL) was added N,N-diisopropylethylamine (0.047 mL, 0.27 mmol), followed by 3,5-dichlorobenzene-1-sulfonyl chloride (50 mg, 0.20 mmol) and the reaction was stirred at ambient temperature for 16 hours. The reaction was then concentrated and purified by preparative reverse phase HPLC to yield 41 mg of N-(4-(4-acetylpiperazin-1-yl)-2-fluorobenzyl)-3,5-dichloro-N-cyclobutylbenzenesulfonamide. 1H NMR (400 MHz, DMSO) δ 7.95 (t, J=1.8 Hz, 1H), 7.72 (d, J=1.8 Hz, 2H), 7.18 (t, J=8.9 Hz, 1H), 6.80-6.74 (m, 1H), 6.74-6.67 (m, 1H), 4.40 (s, 2H), 4.35-4.20 (m, 1H), 3.62-3.51 (m, 4H), 3.25-3.17 (m, 2H), 3.16-3.10 (m, 2H), 2.04 (s, 3H), 2.02-1.88 (m, 4H), 1.55-1.48 (m, 2H); LCMS (m/z) ES+ 514.0 [M+1]+.

1. concentrationThe reaction was then concentrated
2. custompurified by preparative reverse phase HPLC