3-Aminobenzyl alcohol → 1-(4-(3-(hydroxymethyl)phenylamino)-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. (3-aminophenyl)methanol (8.62 mg, 0.07 mmol) was added to the funnel and the plate was left to shake overnight at 80° C. before it was filtered and purified by preparative HPLC to give 1-(4-(3-(hydroxymethyl)phenylamino)-2-(4-(oxazol-5-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)ethanone (7.2 mg, 22%).

Provenance & Evidence