4-Methylmorpholine → 4-[3-(3-Trifluoromethoxy-benzoylamino)-benzylamino]-quinazoline-8-carboxylic acid amide

Participants

Reaction Steps

22.3 mg (0.1 mmol) 4-trifluoromethoxy-benzoic acid were dissolved in 1 ml DMF. 41.8 mg (0.2 mmol) EDCI, 15.0 mg (0.1 mmol) HOBt and 48.5 μl (0.4 mmol) 4-methylmorpholine were added and the mixture was stirred for 15 min. Subsequently, 50 mg (0.1 mmol) 4-(2-Amino-benzylamino)-quinazoline-8-carboxylic acid amide were added and the mixture was stirred overnight at room temperature. The reaction mixture was purified using preoperative HPLC and converted into the hydrochloride salt by treatment with excess HCl in methanol. 18.3 mg, off-white solid.

Provenance & Evidence