2-(Trifluoromethyl)benzylamine → HCID 58447251, compound

Participants

Reaction Steps

A mixture 6-bromo-4-chloro-2H-phthalazin-1-one (100 mg, 0.385 mmol), 2-(trifluoromethyl)benzylamine (0.31 mL, 0.424 mmol), Pd2(dba)3 (35 mg, 0.0385 mmol), rac-BINAP (81 mg, 0.120 mmol) and NaOt-Bu (92 mg, 0.963 mmol) in DMA (6 mL) was heated at 80° C. for 1 h. The mixture was allowed to cool, diluted with EtOAc and washed with water. The organic layer was washed with sat.aq. NaHCO3, brine and dried (Na2SO4). Chromatography on silica (EtOAc/hexanes) afforded 4-chloro-6-(2-trifluoromethyl-benzylamino)-2H-phthalazin-1-one (7 mg) as a white solid, 1H (400 MHz, CDCl3) δ: 4.63 (s, 2H), 6.84 (d, 1H), 6.97 (m, 1H), 7.35 (m, 1H), 7.43 (d, 1H), 7.47 (t, 2H), 8.09 (d, 1H), 10.15 (s, 1H) ppm. m/z (M+1) 353.97.

Provenance & Evidence