反应详情

A mixture of 4-{2-[({[(4-methylphenyl)sulfonyl]amino}carbonyl)oxy]ethyl}phenylboronic acid (100 mg, 0.28 mmol), 5,6-dimethylbenzimidazole (40 mg, 0.28 mmol), Cu(OAc)2 (60 mg, 0.33 mmol), triethylamine (115 μl, 0.83 mmol), MS4A (100 mg), and CH2Cl2 (4 ml) was stirred at room temperature for 1 week. After filtration through a bed of celite, the filtrate was diluted with CH2Cl2, and washed with water. The organic fraction was dried over MgSO4 and filtered. After concentration under reduced pressure, the residue was purified by preparative TLC (CH2Cl2/MeOH=10/1) to afford 28 mg (22%) of the title compound.

1. filtrationAfter filtration through a bed of celite
2. additionthe filtrate was diluted with CH2Cl2
3. washwashed with water
4. dry with materialThe organic fraction was dried over MgSO4
5. filtrationfiltered
6. concentrationAfter concentration under reduced pressure
7. customthe residue was purified by preparative TLC (CH2Cl2/MeOH=10/1)