Water → tert-butyl 4-[({2-tert-butyl-4-[(1,3-oxazol-2-ylmethyl)amino]pyrimidin-5-yl}carbonyl)(2-methylpropyl)amino]-3,4-dihydroisoquinoline-2(1H)-carboxylate

Participants

Reaction Conditions

Reaction Steps

tert-Butyl 4-{[(2-tert-butyl-4-chloropyrimidin-5-yl)carbonyl](2-methylpropyl)amino}-3,4-dihydroisoquinoline-2(1H)-carboxylate (100 mg), 1-(1,3-oxazol-2-yl)methanamine hydrochloride (54 mg) and diisopropylethylamine (0.14 ml) were dissolved in 2-propanol (2 ml), and the mixture was stirred at 80° C. for 6 hr. The reaction mixture was poured into water, and the mixture was extracted with ethyl acetate. The extract was washed with brine, and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure. The residue was subjected to silica gel column chromatography, and the fraction eluted with hexane-ethyl acetate (3:1) was concentrated under reduced pressure to give the object compound (85 mg).

Provenance & Evidence