反应详情

A mixture of 8-[(4-bromophenyl)methyl]-2-hydroxymethyl-6-methyl-5,8-dihydro-6H-pyrido[2,3-d]pyrimidin-7-one (0.95 g, 2.62 mmol), 2-[(1-tert-butyl)-1H-tetrazol-5-yl]phenylboronic acid (0.72 g, 2.90 mmol) (prepared according to J. W. Ellingboe, et al. U.S. Pat. No. 5,149,699), 2M Na2CO3 (5.5 mL), tetrakis(triphenylphosphine)palladium(0) (100 tug, 0.086 mmol), EtOH (3 mL)and toluene (16 mL) was heated under reflux for 20 h. The mixture was diluted with CH2Cl2 and the layers were separated. The organic phase was dried (MgSO4) and concentrated to give an orange oil. Purification by flash chromatography (4% MeOH/CH2Cl2) gave 1.20 g (90%) of product as a colorless foam.

1. customprepared
2. temperatureunder reflux for 20 h
3. customthe layers were separated
4. dry with materialThe organic phase was dried (MgSO4)
5. concentrationconcentrated
6. customto give an orange oil
7. customPurification by flash chromatography (4% MeOH/CH2Cl2)