Dimethylformamide → 2-(1-(bis(tert-butoxycarbonyl)amino)isoquinolin-6-ylamino)-2-[4-(2-hydroxy-butyl)-phenyl]-N-(3-nitro-benzyl)-acetamide

Participants

Reaction Steps

70E (140 mg, 0.25 mmol) was mixed with 3-cyanobenzylamine hydrochloride (57 mg, 0.3 mmol), PyBOP (156 mg, 0.3 mmol), TEA (76 mg, 0.75 mmol) in DMF (3 mL) and stirred at rt for 16 h. The mixture was diluted with H2O and extracted with EtOAc (3×20 mL). The organic layer washed with brine, dried (Na2SO4) and concentrated. Purification via flash chromatography (0-80% EtOAc/hexanes) afforded 70F (180 mg, 63%). MS (ESI) m/z 700.8 (M+H)+.

Provenance & Evidence