反应详情

A mixture of 2-phenyl-pyrimidine-5-carboxylic acid, (80 mg), 1-hydroxybenzotriazole (92 mg) and polymer supported-carbodiimide (640 mg, 1.25 mmol/g) in 8 mL of DCM is shaken at room temperature for 30 min and benzylamine (43 mg) is added. After shaking at room temperature for 1.5 days, PS-trisamine (295 mg, 4.08 mmol/g) is added. The mixture is continually shaken at room temperature for 16 hours. The solid is filtered and washed with DCM. The filtrate is concentrated to yield of 2-phenyl-pyrimidine-5-carboxylic acid benzylamide (98 mg, 85%) as a solid. MS: 290 (M+H); 1H NMR (CDCl3): 9.17 (s, 2H), 8.50 (d, 2H), 7.52-7.55 (m, 3H), 7.36-7.40 (m, 5H), 6.54 (broad, H), 4.69-4.71 (d, 2H); IC50=10 nM.

1. stirringAfter shaking at room temperature for 1.5 days
2. stirringThe mixture is continually shaken at room temperature for 16 hours
3. filtrationThe solid is filtered
4. washwashed with DCM
5. concentrationThe filtrate is concentrated to yield of 2-phenyl-pyrimidine-5-carboxylic acid benzylamide (98 mg, 85%) as a solid