Methanesulfonyl chloride → HCID 56963255, compound

Participants

Reaction Steps

To a solution of 2-(4-bromophenyl)-5-cyclopropyl-N-methyl-6-[(methylsulfonyl)(pyrrolidin-3-yl)amino]-2H-indazole-3-carboxamide in DCM at 0° C. was added DIPEA (4 μL, 0.023 mmol), followed by methanesulfonyl chloride (3 μL, 0.039 mmol) and the mixture was stirred at RT for 20 min. The mixture was concentrated to dryness and purified by preparative LCMS (5-40-100% ACN in 0.1% aqueous formic acid) to afford Compound (52) as a white solid (1.4 mg, 36%). ESI-MS m/z calculated for [M+H]+: 610.1/612.1; found: 610.0/612.0; 1H NMR (400 MHz, CDCl3) δ 7.72 (2×s, 1H), 7.70-7.64 (m, 2H), 7.51-7.44 (m, 2H), 7.36 (2×s, J=2.6 Hz, 1H), 5.75 (2×d, J=5.0 Hz, 1H), 4.92-4.68 (m, 1H), 3.88-3.68 (m, 1H), 3.54-3.37 (m, 1H), 3.38-3.16 (m, 2H), 3.10 (d, J=4.6 Hz, 3H), 3.00 (2×d, 3H), 2.79 (2×s, 3H), 2.43-2.17 (m, 2H), 2.17-1.82 (m, 1H), 1.21-0.95 (m, 3H), 0.80-0.62 (m, 1H).

Provenance & Evidence