反应详情

温度

55 °C

Compound 78 (127 mg, 0.336 mmol) was reduced to 79 by hydrogenation according to general procedure A in example 10. A mixture of above amine DS13a and 1H-indole-2,5-dicarboxylic acid bis-(pentafluorophenyl-amide) 74 (45 mg, 0.084 mmol) in 2 ml of anhydrous DMF under argon was stirred at 55° C. overnight. The solvent was evaporated to dryness. The residue was dissolved in 5 ml of TFA/anisole (8:2) and the mixture was kept at room temperature for 1 h. The product was precipitated by ether and purified by HPLC described in general procedure B in example 10 to give 76 (22 mg, 40%). ESI MS: 662.27 (M+H+), 331.64 (M/2+H+).

1. customThe solvent was evaporated to dryness
2. dissolutionThe residue was dissolved in 5 ml of TFA/anisole (8:2)
3. waitthe mixture was kept at room temperature for 1 h
4. customThe product was precipitated by ether
5. custompurified by HPLC