反应详情

温度

90 °C

To a mixture of 2,6-dicyanobenzene boronic acid (0.516 g) and anhydrous K2CO3 (0.2 g) in toluene (10 mL) under N2 was added N-(2,6-dichlorobenzoyl)-O-(trifluoromethanesulfonyl)-L-tyrosine methyl ester (0.5 g). Pd(PPh3)4 (0.1 g) was added and the mixture was heated at 90° C. for 8 h. The mixture was cooled, diluted with EtOAc and washed successively with water and brine. The organic layer was dried (MgSO4) and evaporated, and the residue was purified by column chromatography (silica gel; eluent: EtOAc/hexane 1/1) to yield 58 mg of N-(2,6-dichlorobenzoyl)-4-(2,6-dicyanophenyl)-L-phenylalanine methyl ester.

1. temperatureThe mixture was cooled
2. washwashed successively with water and brine
3. dry with materialThe organic layer was dried (MgSO4)
4. customevaporated
5. customthe residue was purified by column chromatography (silica gel; eluent: EtOAc/hexane 1/1)