Diisopropylethylamine → Tert-butyl (1-(4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)phenylsulfonylcarbamoyl)cyclopropyl)methylcarbamate

Participants

Reaction Steps

To a solution of 4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)benzenesulfonamide (1 g, 1.94 mmol) in DCM (10 mL) solution were added PyBOP (1.21 g, 2.33 mmol), 1-((tert-butoxycarbonylamino)methyl)cyclopropanecarboxylic acid (0.46 g, 2.14 mmol) and DIEA (1.36 mL, 7.77 mmol). The mixture was stirred at room temperature for 16 hs. All solvents were removed under vacuum and the residue was purified by silica gel column (MeOH/hexane: 5%) to give tert-butyl (1-(4-(4-(1-(4-chlorophenyl)cyclopropylamino)-6-(2,2,2-trifluoroethoxy)-1,3,5-triazin-2-ylamino)phenylsulfonylcarbamoyl)cyclopropyl)methylcarbamate (1.38 g, 100%) as a brown solid. LC-MS (Condition A), MS m/z 712.0 (M++H).

Provenance & Evidence