反应详情

To a solution of 5-(4-methoxy-benzoylamino)-3,3-dimethyl-6-nitro-2-oxo-2,3-dihydro-indole-1-carboxylic acid 4-nitro-phenyl ester (54 mg) in CH2Cl2 (10 ml) is added benzyl amine (44 μl) at RT. The reaction mixture is stirred at RT for 20 h. After an aqueous work-up and concentration in vacuo, the residue is dissolved in acetic acid (3 ml) and iron (60 mg; powder) is added. The mixture is stirred in a microwave apparatus at 150° C. for 900 s. After filtration and evaporation of the solvent the crude material is purified by preparative RP-HPLC.

1. concentrationAfter an aqueous work-up and concentration in vacuo
2. dissolutionthe residue is dissolved in acetic acid (3 ml)
3. additioniron (60 mg; powder) is added
4. stirringThe mixture is stirred in a microwave apparatus at 150° C. for 900 s
5. filtrationAfter filtration and evaporation of the solvent the crude material
6. customis purified by preparative RP-HPLC