反应详情

6-(Trifluoromethyl)nicotinic acid (Sigma-Aldrich; 178 mg, 0.934 mmol) was stirred in DCM (10 mL). Oxalyl chloride (0.131 mL, 1.494 mmol) then DMF (2.89 μl, 0.037 mmol) were added and the reaction mixture was left to stir at room temperature for 2 hrs under Argon. The reaction mixture was evaporated to dryness and the resulting residue was dissolved in DCM (10 mL). A solution of [(2-trifluoromethyl-1H-indol-5-yl)methyl]amine (Intermediate 4, 160 mg, 0.747 mmol) in DCM (10 mL) was added followed by triethylamine (0.208 mL, 1.494 mmol). The reaction mixture was left to stir at room temperature for 1 h. The reaction mixture was evaporated to dryness and the resulting residues where purified by MDAP to give the title compound (176 mg);

1. waitthe reaction mixture was left
2. customThe reaction mixture was evaporated to dryness
3. dissolutionthe resulting residue was dissolved in DCM (10 mL)
4. waitThe reaction mixture was left
5. stirringto stir at room temperature for 1 h
6. customThe reaction mixture was evaporated to dryness
7. customthe resulting residues where purified by MDAP