Methanol → HCID 49855065, compound

Participants

Reaction Steps

To a solution of 1-(4-(3-acetyl-6-(methoxymethyl)-3-aza-bicyclo[3.1.0]hexan-1-yl)phenyl)pyrrolidin-2-one (360 mg, 1.097 mmol) obtained in Step 1 of Example XXXIV, in dry THF (10 mL), was added BF3.OEt2 (0.027 mL, 0.21 mmol) at 40° C. The reaction mixture was heated at the same temperature for 20 min followed by the addition of BH3.Me2S (2.79 mL, 5.48 mmol, 2M solution). Reaction mixture was heated to reflux for 6 h. After the completion of the reaction as confirmed by TLC, methanol (15 mL) was added to the cold solution and refluxed further for 1 h. The solvents were removed in vacuo to afford the crude compound, which was purified by column chromatography (silica gel, 1:9 MeOH:DCM) to afford pure title compound (150 mg, 45%).

Provenance & Evidence