反应详情

TBTU (40 mg, 0.125 mmol) in 0.25 mL DMF was added to 2-chloro-5-(tert-butylcarbonylamino)methyl-benzoic acid (34 mg, 0.125 mmol), followed by 50 μL TEA and the mixture was stirred for 5 min. Then N-(4-bromophenyl)-2-methoxy-5-amino-benzoic acid amide in 0.25 mL DMF was added and it was stirred overnight. The crude mixture was filtered through aluminium oxide and the solid phase was washed 4× with 1 mL DMF/MeOH 9:1. The combined organic phase was concentrated i.vac. dissolved in Acetonitrile/HCOOH, filtered and dried via lyophilisation to furnish the title compound.

1. stirringit was stirred overnight
2. filtrationThe crude mixture was filtered through aluminium oxide
3. washthe solid phase was washed 4× with 1 mL DMF/MeOH 9:1
4. concentrationThe combined organic phase was concentrated i.vac
5. dissolutiondissolved in Acetonitrile/HCOOH
6. filtrationfiltered
7. customdried via lyophilisation