Oxalyl chloride → 6-Chloro-2-fluoro-3-((3-hydroxy-2,2-dimethylpropanamido)methyl)-N-(4-(3-(trifluoromethyl)phenoxy)quinazolin-8-yl)benzamide

Participants

Reaction Steps

The title compound was prepared following the procedure described in Example-1 using 4-(3-(trifluoromethyl)phenoxy)quinazolin-8-amine (Intermediate-8, 200 mg, 0.655 mmol), 6-chloro-2-fluoro-3-((3-hydroxy-2,2-dimethylpropanamido)methyl)benzoic acid (Intermediate-59, 237 mg, 0.78 mmol), oxalyl chloride (166 mg, 1.32 mmol), DMF (1 drop) and DIPEA (253 mg, 1.96 mmol) in CH2Cl2 (3 mL) to afford 10 mg of the title product. 1H NMR (300 MHz, DMSO-d6): δ 10.94 (s, 1H), 8.88 (d, 1H), 8.77 (s, 1H), 8.14 (m, 2H), 7.85 (m, 2H), 7.73 (s, 3H), 7.36 (m, 2H), 4.91 (t, 1H), 4.31 (d, 2H), 3.40 (m, 2H), 1.06 (s, 6H); MS [M+H]+: 591.29.

Provenance & Evidence