3-(Cyclopropylamino)propionitrile → tert-Butyl 4-((2-cyanoethyl)(cyclopropyl)amino)-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate

Participants

Reaction Conditions

Reaction Steps

tert-Butyl 2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-4-(trifluoromethylsulfonyloxy)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carboxylate (250 mg, 0.45 mmol, example 69c) was dissolved in DMF (2 mL). 3-(cyclopropylamino)propanenitrile (49.7 mg, 0.45 mmol) was added and the reaction mixture was stirred at 85° C. overnight. The mixture was allowed to reach room temperature and the solvent was evaporated under reduced pressure. The crude tert-butyl 4-((2-cyanoethyl)(cyclopropyl)amino)-2-(4-(2-methyl-1H-imidazol-1-yl)phenylamino)-7,8-dihydropyrido[4,3-d]pyrimidine-6 (5H)-carboxylate (241 mg, 104%) was used as such in the subsequent step.

Provenance & Evidence