反应详情

A mixture of (R)-5-chloro-6-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 38.1, 50 mg, 0.124 mmol), (2-aminopyrimidin-5-yl)boronic acid (26 mg, 0.187 mmol), 2 M Na2CO3 (0.124 mL, 0.249 mmol) and DME (2.5 mL) was flushed with argon and PdCl2(dppf)(CH2Cl2) (10 mg, 0.012 mmol) was added. The mixture was subjected to MW irradiation 140° C. for 30 min, passed through a PL-Thiol MP SPE cartridge (StratoSpheres™), the cartridge was washed with MeOH and the solvent was evaporated off under reduced pressure to give a residue which was purified by preparative LC-MS to afford the title compound. LC-MS (Condition 5) tR=1.53 min, m/z=461.1 [M+H]+, m/z=459.1 [M−H]−.

1. additionwas added
2. customThe mixture was subjected to MW irradiation 140° C. for 30 min
3. washthe cartridge was washed with MeOH
4. customthe solvent was evaporated off under reduced pressure
5. customto give a residue which
6. customwas purified by preparative LC-MS