反应详情

温度

70 °C

Under argon atmosphere, a solution of 1.75 g of (1R,2S)-N-tert-butoxycarbonyl-2-(2-chloro-6-methoxyquinazolin-4-yl)aminocyclohexylamine and 1.47 g of 4-methoxybenzylamine in 100 mL of anhydrous toluene was combined with 97 mg of palladium acetate, 268 mg of 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl and 1.03 g of sodium tert-butoxide, and stirred at 70° C. for 5 hours. The reaction solvent was concentrated, and then combined with water, extracted with chloroform, and dried. After the solvent was distilled off, the residue was purified by column chromatography on silica gel (chloroform:methanol=20:1) to obtain 1.62 g of the desirable compound.

1. concentrationThe reaction solvent was concentrated
2. extractionextracted with chloroform
3. customdried
4. distillationAfter the solvent was distilled off
5. customthe residue was purified by column chromatography on silica gel (chloroform:methanol=20:1)