反应详情

2-(2-Bromo-1-methyl-4-phenyl-1H-imidazol-5-yl)[1,3]thiazolo[5,4-d]pyrimidin-7-amine (Example 26) (20 mg), PdCl2dppf (8 mg), pyridine-4-boronic acid (8 mg) and 2M sodium carbonate (2.0 mL) were heated in DMF (2.0 mL) at 100° C. under an inert atmosphere. After 3 hours the reaction mixture was cooled to ambient temperature, EtOAc (25 mL) added then washed with water (15 mL), brine (2×10 mL), dried (MgSO4), filtered and concentrated in vacuo. Purification by flash chromatography on silica eluting with 6% MeOH/DCM gave a dark brown solid which was washed with diethyl ether then dried under high vacuum to give the title compound as light brown solid (6 mg, 31%);

1. washthen washed with water (15 mL), brine (2×10 mL)
2. dry with materialdried (MgSO4)
3. filtrationfiltered
4. concentrationconcentrated in vacuo
5. customPurification by flash chromatography on silica eluting with 6% MeOH/DCM
6. customgave a dark brown solid which
7. washwas washed with diethyl ether
8. customthen dried under high vacuum