(1R,3S,5R)-2-[2-(3-Acetyl-5-benzyloxy-indazol-1-yl)-acetyl]-2-aza-bicyclo[3.1.0]hexane-3-carboxylic acid (2-fluoro-3-trifluoromethoxy-phenyl)-amide → (1R,3S,5R)-2-[2-(3-Acetyl-5-hydroxy-indazol-1-yl)-acetyl]-2-aza-bicyclo[3.1.0]hexane-3-carboxylic acid (2-fluoro-3-trifluoromethoxy-phenyl)-amide

Participants

Reaction Steps

A mixture of (1R,3S,5R)-2-[2-(3-acetyl-5-benzyloxy-indazol-1-yl)-acetyl]-2-aza-bicyclo[3.1.0]hexane-3-carboxylic acid (2-fluoro-3-trifluoromethoxy-phenyl)-amide (2.0 g, 3.28 mmol) and Pd/C (10%, 165 mg) in MeOH (40 mL) was stirred under a H2 atmosphere for 1 h. The mixture was filtered through a celite pad and concentrated. The product was used in the next step without further purification. MS (UPLC-MS): 521 [M+H]+; tR (HPLC conditions f): 2.02 min.

Provenance & Evidence