反应详情

To a solution of (3-acetyl-5-benzyloxy-indazol-1-yl)-acetic acid (1.38 g, 4.30 mmol, prepared as described in Part A), (1R,3S,5R)-2-aza-bicyclo[3.1.0]hexane-3-carboxylic acid (2-fluoro-3-trifluoro methoxy-phenyl)-amide trifluoroacetate (1.80 g, 4.30 mmol) and propylphosphonic anhydride (50% in EtOAc, 3.80 ml, 6.46 mmol) in CH2Cl2 (40 ml) was added DIPEA (2.25 mL, 12.91 mmol) and the resulting mixture was stirred at RT for 2 h. The mixture was concentrated and the crude residue was purified by flash column chromatography on silica gel (c-hexane/EtOAc 1:0 to 0:1). MS (UPLC-MS): 611 [M+H]+; tR (HPLC conditions f): 2.40 min.

1. concentrationThe mixture was concentrated
2. customthe crude residue was purified by flash column chromatography on silica gel (c-hexane/EtOAc 1:0 to 0:1)
3. custom2.40 min.