反应详情

A mixture, comprising 3-amino-6-bromo-5-trifluoromethyl-pyrazine-2-carboxylic acid (Intermediate 2)(0.349 g, 1.221 mmol), 3-(piperidin-1-ylmethyl)-1H-pyrazol-5-amine (Intermediate 8) (0.220 g, 1.221 mmol), HATU (0.464 g, 1.221 mmol) and N-methylmorpholine (0.241 ml, 2.441 mmol) in DMF (5 ml) was stirred for 30 minutes at RT. The reaction mixture was diluted with water (20 ml) and the resulting yellow precipitate was filtered under vacuum and washed with water (20 ml). The resulting residue was loaded onto a SCX-2 cartridge eluting with MeOH followed by 7M NH3 in MeOH. The methanolic ammonia fractions were concentrated in vacuo and the residue was triturated with EtOAc/iso-hexane to yield the title compound.

1. filtrationthe resulting yellow precipitate was filtered under vacuum
2. washwashed with water (20 ml)
3. washeluting with MeOH
4. concentrationThe methanolic ammonia fractions were concentrated in vacuo
5. customthe residue was triturated with EtOAc/iso-hexane