反应详情

2-(Trifluoromethyl)-5-pyrimidinecarboxylic acid (Bio-Farma) (108 mg, 0.560 mmol) was stirred in dichloromethane (10 ml). Oxalyl chloride (0.082 ml, 0.934 mmol) then DMF (1.808 μl, 0.023 mmol) was added. The reaction mixture was then left to stir for 2 h under Argon gas. The reaction mixture was then evaporated to dryness and the resulting residues were then dissolved in dichloromethane (10 ml). A solution of {[2-(trifluoromethyl)-1H-indol-5-yl]methyl}amine (Intermediate 4, 100 mg, 0.467 mmol) in DCM (10 mL) was added then triethylamine (0.130 ml, 0.934 mmol) was added. The reaction mixture was then left to stir at room temperature for 1 h. The reaction mixture was evaporated to dryness. The resulting residues where then purified on the MDAP to give the title compound (105 mg). m/z (ES+) 389 (M+1); 1H NMR (400 MHz, d6-DMSO): δ 12.24 (1H, s), 9.57 (1H, t), 9.43 (2H, s), 7.68 (1H, s), 7.45 (1H, d), 7.32 (1H, dd), 7.00 (1H, s), 4.63 (2H, d).

1. waitThe reaction mixture was then left
2. customThe reaction mixture was then evaporated to dryness
3. dissolutionthe resulting residues were then dissolved in dichloromethane (10 ml)
4. waitThe reaction mixture was then left
5. stirringto stir at room temperature for 1 h
6. customThe reaction mixture was evaporated to dryness
7. customThe resulting residues where then purified on the MDAP