反应详情

Anisole (0.027 ml, 0.244 mmol) and 25% TFA in dichloroethane (2 ml, 6.49 mmol) were added to methyl 5-(2-chloro-5-cyano-3-((7-cyano-4-(cyclopropyl(4-methoxybenzyl)amino)imidazo[2,1-f][1,2,4]triazin-2-yl)amino)phenyl)octahydro-1H-pyrrolo[3,2-c]pyridine-1-carboxylate (28 mg, 0.0429 mmol) and the resulting solution was stirred at room temperature over the weekend. Solvent was evaporated in vacuo and the residue was dissolved in acetonitrile and neutralized with 2N ammonia in methanol. Desired product precipitated and was collected by filtration, methyl 5-(2-chloro-5-cyano-3-((7-cyano-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazin-2-yl)amino)phenyl)octahydro-1H-pyrrolo[3,2-c]pyridine-1-carboxylate (17.2 mg) was obtained as a white solid.

1. customSolvent was evaporated in vacuo
2. dissolutionthe residue was dissolved in acetonitrile and neutralized with 2N ammonia in methanol
3. customDesired product precipitated
4. filtrationwas collected by filtration