Cyclopropylamine → Cyclopropyl-4-[2-(4-fluorophenyl)-8-methylimidazo[1,2-a]pyrazin-3-yl]-pyrimidin-2-ylamine

Participants

Reaction Conditions

Reaction Steps

To a mixture of 2-(4-fluorophenyl)-3-(2-methanesulfonylpyrimidin-4-yl)-8-methylimidazo[1,2-a]pyrazine (Example #G.1; 3.66 g, 9.55 mmol) in ACN (70 mL) was added cyclopropylamine (3.31 mL, 47.7 mmol). The mixture was heated to about 80° C. After about 16 h, the mixture was treated with additional cyclopropylamine (3.0 mL, 43 mmol) and heated at about 80° C. for about another 4 h. The mixture was cooled to ambient temperature and filtered. The resulting solid was washed with ACN and dried to yield the title compound as a white solid (2.85 g, 83%): LC/MS (Table 1, Method b) Rt=2.0 min; MS m/z: 361.2 (M+H)+.

Provenance & Evidence