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-fluoropyridin-3-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. PdCl2(dppf)(CH2Cl2) (10 mg, 0.012 mmol) was added and the mixture was subjected to MW irradiation 140° C. for 30 min, filtered through a PL-Thiol MP SPE cartridge (StratoSpheres™, 6 mL), 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 6) tR=1.71 min, m/z=463.0 [M+H]+.

1. customwas flushed with argon
2. customthe mixture was subjected to MW irradiation 140° C. for 30 min
3. filtrationfiltered through a PL-Thiol MP SPE cartridge (StratoSpheres™, 6 mL)
4. washthe cartridge was washed with MeOH
5. customthe solvent was evaporated off under reduced pressure
6. customto give a residue which
7. customwas purified by preparative LC-MS