Morpholine → 6-Bromo-1-morpholinophthalazine

Participants

Reaction Conditions

Reaction Steps

A mixture of 6-bromo-1-chlorophthalazine (Example 1, 0.1 g, 411 μmol), morpholine (72 mg, 821 μmol) and potassium carbonate (57 mg, 411 μmol) in 5 mL acetonitrile was added to a glass microwave reaction vessel. The reaction mixture was stirred and heated in a Smith Synthesizer® microwave reactor (Personal Chemistry, Inc., Upssala, Sweden) at 180° C. for 20 min. All the starting material was converted to product (M+1=296, 298). The mixture was concentrated under vacuum, and purified via flash chromatography (silica gel) eluting with a gradient of 2% 2 M ammonia in MeOH/DCM to 6% 2 M ammonia in MeOH/DCM to give 6-bromo-1-morpholinophthalazine as yellow solid. Found MS (ES+): 296, 298(M+H)+.

Provenance & Evidence