Diisopropylethylamine → HCID 59140916, compound

Participants

Reaction Steps

125 mg (0.28 mmol) of 2-[4-(2-carboxy-phenyl)-thiazol-2-ylcarbamoyl]-pyrrolidine-1-carboxylic acid benzyl ester (IS2277-52) was dissolved in 4 mL of DMF. To this solution was added HATU (160.9 mg, 0.42 mmol) and DIEA (0.05 mL, 0.36 mmol). This solution was stirred at room temperature for 1 hour. To this solution was added 56.1 mg (0.28 mmol) of 3-amino-piperidine-1-carboxylic acid tert-butyl ester. Reaction mixture was stirred overnight at room temperature, and then purified using reverse phase HPLC. MS: 634.2 (M+H+); H1 NMR (meOH-d4): δ(ppm) 8.02 (m, 2H), 7.89 (m, 2H), 7.58 (m, 1H), 7.39 (m, 3H), 7.19 (m, 1H), 7.07 (m, 2H), 5.03 (m, 2H), 45.2 (m, 1H), 4.11 (m, 3H), 3.61 (m, 4H), 3.19 (m, 1H), 2.97 (m, 2H), 2.41 (m, 1H), 2.28 (m, 1H), 2.01 (m, 4H), 1.48 (s, 9H).

Provenance & Evidence