Dimethylformamide → HCID 178482419, compound

Participants

Reaction Steps

HATU (10.8 mg, 0.028 mmol, 1.1 equivalents) in DMF (0.2 ml) was added to the solution of cis-4-(4-(azepan-1-yl)-6-(methylamino)-1,3,5-triazin-2-ylamino) cyclohexanecarboxylic acid (8.96 mg, 0.026 mmol, 1 equivalent) in DMF (1 ml), followed by adding DIEA (11.2 μL, 0.064 mmol, 2.5 equivalents). 2-(trifluoromethyl)-benzenemethanamine (5.9 mg, 0.031 mmol, 1.2 equivalents) in DMF (0.1 ml) was added. The reaction solution was stirred at room temperature for 2 hours. LC-MS showed the reaction had 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 final product (˜7.7 mg, 57%). MS (ES+): m/e 522.4 [M+H]+.

Provenance & Evidence