反应详情

4-(tert-Butoxycarbonylamino)tetrahydro-2H-pyran-4-carboxylic acid (374 mg), (S)-2-amino-3-(4′-cyanobiphenyl-4-yl)propanamide (Example 3, step (iii), 405 mg) and N-ethyl-N-isopropylpropan-2-amine (0.664 mL) were dissolved in DMF (10 mL) and to the solution was added TBTU (734 mg). The reaction mixture was stirred at room temperature for 2 days. The reaction mixture was evaporated to dryness, dissolved in dichloromethane (20 mL) and was absorbed onto silica. The product was purified by chromatography on silica eluting with 20% ethyl acetate in isohexane, then 50% ethyl acetate in isohexane and then 100% ethyl acetate to afford after evaporation of the relevant fractions the sub-titled compound (700 mg).

1. customThe reaction mixture was evaporated to dryness
2. dissolutiondissolved in dichloromethane (20 mL)
3. customwas absorbed onto silica
4. customThe product was purified by chromatography on silica eluting with 20% ethyl acetate in isohexane
5. custom50% ethyl acetate in isohexane and then 100% ethyl acetate to afford
6. customafter evaporation of the relevant fractions the sub-titled compound (700 mg)