2,4,5-Trichloropyrimidine → 2-(6-((2,5-Dichloropyrimidin-4-yl)amino)hexahydrofuro[3,2-b]furan-3-yl) isoindoline-1,3-dione

Participants

Reaction Steps

To a solution of 2,4,5-trichloropyrimidine (1.45 g, 7.9 mmol) in MeOH (40 mL) were added triethanamine (970 mg, 9.6 mmol) and 2-(6-aminohexahydrofuro[3,2-b]furan-3-yl)isoindoline-1,3-dione (crude product from above step). The mixture was stirred at room temperature overnight, Then concentrated in vacuo, the residue was purified by silica gel column chromatography (EtOAc/PE (v/v)=1/3) to give the desired compound as a white solid (450 mg, 13.5% three steps).

Provenance & Evidence