Triethylamine → 4-[({4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)(methyl)amino]-1-(methylsulfonyl)piperidine-4-carboxamide

Participants

Reaction Steps

Methanesulfonyl chloride (7.5 μl, 0.094 mmol) was added to a stirred solution of 4-[({4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl}methyl)(methyl)amino]piperidine-4-carboxamide hydrochloride (0.05 g, 0.085 mmol) and triethylamine (53 μl, 0.38 mmol) in dichloromethane (1 ml) at room temperature. The reaction mixture was stirred at room temperature for 1 hour, concentrated and purified by preparative LCMS (standard basic system) to give the title product (0.0107 g, 23%) as a white solid; 1H NMR Spectrum: (DMSO-d6) 1.98 (m, 2H), 2.22 (m, 2H), 2.36 (s, 3H), 2.84 (s, 3H), 2.96 (m, 2H), 3.44 (m, 2H), 3.66 (s, 2H), 3.98 (s, 3H), 7.19 (s, 1H), 7.26-7.30 (m, 3H), 7.52-7.53 (m, 2H), 8.33 (s, 1H), 8.42 (s, 1H), 9.70 (s, 1H); Mass Spectrum: (M+H)+ 551.

Provenance & Evidence