反应详情

温度

140 °C

A mixture of (R)-5-chloro-6-(3-hydroxypyrrolidin-1-yl)-N-(4-(trifluoromethoxy)phenyl)nicotinamide (Stage 12.1, 50 mg, 0.124 mmol), (4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)thiophen-2-yl)methanol (45 mg, 0.187 mmol), 2 M Na2CO3 (0.124 mL, 0.249 mmol) and DME (2.5 mL) were added to a MW vial, which was sealed and evacuated/purged with argon. PdCl2(dppf)-(CH2Cl2) was added (10 mg, 0.012 mmol) and the mixture was stirred at 140° C. for 30 min. The RM was filtered 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 1.55 min, m/z=479.9 [M+H]+.

1. additionwere added to a MW vial, which
2. customwas sealed
3. customevacuated/purged with argon
4. additionPdCl2(dppf)-(CH2Cl2) was added (10 mg, 0.012 mmol)
5. filtrationThe RM was filtered through a PL-Thiol MP SPE cartridge (StratoSpheres™)
6. washthe cartridge was washed with MeOH
7. customthe solvent was evaporated off under reduced pressure
8. customto give a residue which
9. customwas purified by preparative LC-MS