Isopropylamine → 6-[5-[(Cyclopropylamino)carbonyl]-2-methylphenyl]-N-(1-methylethyl)-1-phthalazinecarboxamide

Participants

Reaction Steps

3-(1-Cyanophthalazin-6-yl)-N-cyclopropyl-4-methylbenzamide (115 mg, 350 μmol) and potassium hydroxide (39 mg, 700 μmol) were dissolved in ethanol/water (1:1) (3.50 mL) before it was placed in the microwave for 10 min at 120° C. The reaction mixture was concentrated before it was dissolved in dimethylformamide (700 μl); HATU (266 mg, 700 μmol) and isopropylamine (150 μl, 1751 μmol) were added. This was stirred at RT for 16 h before more HATU was added, and the reaction mixture was stirred at RT for 7 h. The reaction mixture was diluted with 100 mL of ethyl acetate, added to a separatory funnel, partitioned with water, washed 2× with 50 mL of water, separated, dried over sodium sulfate, concentrated in vacuo, and purified by HPLC to give the title compound.

Provenance & Evidence