(2R)-2,3-dihydro-1H-indol-2-ylmethanol → (R)-1-(4-(2-(Hydroxymethyl)indolin-1-yl)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanone

Participants

Reaction Steps

6-Acetyl-2-(4-(oxazol-5-yl)phenylamino)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl trifluoromethanesulfonate (35 mg, 0.07 mmol, Example 26a) in DMSO (1 mL) was dispensed in a library plate. (R)-indolin-2-ylmethanol (10.44 mg, 0.07 mmol) was added to it and the reaction mixture was left to shake overnight at 80° C. before filtered and purified by preparative HPLC to yield (R)-1-(4-(2-(Hydroxymethyl)indolin-1-yl)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanone (12.7 mg, 36%).

Provenance & Evidence