Ammonium formate → (1S,2S,5R)-2-(7,7-difluoro-3-azabicyclo[3.3.0]oct-2-ylmethyl)-isoindole-1,3-dione

Participants

Reaction Steps

To a suspension of (1S,2S,5R)-2-(3-benzyl-7,7-difluoro-3-azabicyclo[3.3.0]oct-2-ylmethyl)-isoindole-1,3-dione (1.73 g), Pd—C 10% (1.7 g) in dry MeOH (146 mL) was added ammonium formate (1.38 g). The reaction mixture was stirred at reflux for 16 h, cooled to RT and filtered over a pad of celite. The filtrate was concentrated in vacuo, partitioned between DCM/water. The aqueous phase was concentrated to yield 0.8 g (60%) of the title compound as a white solid

Provenance & Evidence