反应详情

温度

120 °C

2-Methyl-N-[6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indazol-4-yl]-1,3-thiazole-4-carboxamide (23 mg, 0.06 mmol), 5-bromo-3-pyridinesulfonamide (18 mg, 0.078 mmol) and Pd(PPh3)4 (7 mg, 0.006 mmol) were combined in IPA (0.5 ml) and 1 M sodium bicarbonate (aq) (0.18 ml). The reaction was heated in a Biotage microwave at 120° C. for 10 mins. After cooling the solvent was removed under a stream of nitrogen and the solid partitioned between water (10 ml) and ethyl acetate:DCM (3×10 ml, 1:1, v/v). A few drops of brine were added to aid separation. The organic layers were combined, passed through a hydrophobic frit and dried under a stream of nitrogen. The residue was dissolved in MeOH:DMSO (0.5 ml, 1:1, v/v) and purified by MDAP (Method B). The solvent was removed under a stream of nitrogen to give the title compound, 1.5 mg.

1. temperatureAfter cooling the solvent
2. customwas removed under a stream of nitrogen
3. customthe solid partitioned between water (10 ml) and ethyl acetate
4. additionA few drops of brine were added
5. customseparation
6. customdried under a stream of nitrogen
7. dissolutionThe residue was dissolved in MeOH
8. customDMSO (0.5 ml, 1:1, v/v) and purified by MDAP (Method B)
9. customThe solvent was removed under a stream of nitrogen