反应详情

A mixture of 7-(2-amino-benzoylamino)-4,4-dimethyl-3,4-dihydro-1H-isoquinoline-2-carboxylic acid tert-butyl ester (512 mg, 1.3 mmol), pyridazine-4-carbaldehyde (140 mg, 1.3 mmol) and p-toluenesulfonic acid (10 mg) was heated at reflux in toluene (5 mL) for 1 h. The mixture was cooled to RT and diluted with CH2Cl2. NaBH4 (50 mg, 1.3 mmol) was added to the mixture followed by MeOH (2 mL). The mixture was stirred for 1 h. The crude material was purified with flash chromatography (SiO2, 5% MeOH/CH2Cl2) to give a yellow solid. MS (ES+): 488.0 (M+H)+. Calc'd for C28H33N5O3: 487.59.

1. temperaturewas heated
2. customThe crude material was purified with flash chromatography (SiO2, 5% MeOH/CH2Cl2)
3. customto give a yellow solid