(2R)-2,3-dihydro-1H-indol-2-ylmethanol → (R)-(1-(6-methyl-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)indolin-2-yl)methanol

Participants

Reaction Steps

6-Methyl-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl trifluoromethanesulfonate (65 mg, 0.14 mmol, Example 9a) and (R)-indolin-2-ylmethanol (20.70 mg, 0.14 mmol) in DMSO (3 mL) were heated to 80° C. in a microwave reactor for 2 h. The reaction mixture was filtered and purified by preparative HPLC, yielding (R)-(1-(6-methyl-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)indolin-2-yl)methanol (31.0 mg, 47.8%).

Provenance & Evidence