Octahydropyrrolo[1,2-a]piperazin-6-one → 2-(6-chlorophthalazin-1-yl)-tetrahydropyrrolo[1,2-a]pyrazin-6(1H,2H,7H)-one

Participants

Reaction Conditions

Reaction Steps

A mixture of tetrahydropyrrolo[1,2-a]pyrazin-6(1H,2H,7H)-one (Med. Chem. Res., 7:301 (1997); 0.983 g, 7.01 mmol), 1,6-dichlorophthalazine (1.36 g, 6.83 mmol) and TEA (2.00 mL, 14.3 mmol) in 18 mL of CH3CN was heated at 135° C. for 30 min in a microwave oven. The reaction mixture was concentrated onto silica gel and purified using flash chromatography eluting with 2M NH3 in MeOH:CH2Cl2 (0:1→3:97) to give 404 mg (20%) an orange foam/amorphous solid. MS m/z: 303.1 [M+1].

Provenance & Evidence