HATU (17.4 mg, 0.046 mmol, 1.1 equivalents) in DMF (0.2 ml) was added to the solution of cis-4-(4-amino-6-(azepan-1-yl)-1,3,5-triazin-2-ylamino)cyclohexanecarboxylic acid (13.9 mg, 0.042 mmol, 1 equivalent) in DMF (1 ml), followed by adding DIEA (18.1 ul, 0.104 mmol, 2.5 equivalents). 2-(trifluoromethyl)-benzenemethanamine (9.54 mg, 0.05 mmol, 1.2 equivalents) in DMF (0.1 ml) was added. The reaction solution was stirred at room temperature for 2 hrs. LC-MS showed the reaction has completed. The reaction was diluted with EtOAc (2 ml), which was further washed with water (2×1.5 ml). The organic layer was dried and purified by RP-HPLC (Luna 5μ C8(2), 100×21 mm, 25-80% CH3CN/H2O, 0.1% TFA, 20 min) to give the desired product (12.2 mg, 58%). MS (ES+): m/e 508.4 [M+H]+.
