Isobutyric Acid → HCID 66802656, compound

Participants

Reaction Steps

To 2-methylpropanoic acid (27.0 μL, 0.299 mmol) in DMF (5 mL) was added DIPEA (109 μL, 0.624 mmol) at room temperature and the mixture was stirred for 5 min. (1H-Benzotriazol-1-yloxy)[tris(dimethylamino)]phosphonium hexafluorophosphate (0.121 g, 0.274 mmol) was added to the reaction mixture and stirred for 5 min. 2-N-Methyl-2-N-phenyl-6-[5-(piperidin-4-yl)-1,2,4-oxadiazol-3-yl]-1,3,5-triazine-2,4-diamine hydrochloride (Intermediate 105, 0.100 g, 0.249 mmol) was added and the mixture was stirred at room temperature for 18 h. The reaction mixture was diluted with water, extracted with EtOAc and the organic layer washed with brine. The combined organic extracts were dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The crude compound was purified by FCC (DCM:MeOH 90:10) to afford the title compound (96 mg, 88%).

Provenance & Evidence