Dimethylformamide → HCID 59367659, compound

Participants

Reaction Steps

The crude 2-(6-Morpholin-4-yl-3-azabicyclo[3.1.0]hex-3-yl)pyrimidine-5-carboxylic acid was suspended in anhydrous DMF (3 ml) and EDCl (19 mg, 0.1 mmol) and HOBt (11 mg, 0.075 mmol) were added. After stirring for ˜5 minutes, triethylamine (35 μl, 0.25 mmol) and intermediate D (58 μl, 0.5 mmol) were added and the resultant mixture was stirred at r.t. for 18 h. The reaction mixture was diluted with water and extracted with EtOAc (3×10 ml) and DCM (2×10 ml). The combined organics were dried (MgSO4) and evaporated onto silica. The residue was purified by flash chromatography eluting with 100% DCM to 15% MeOH/DCM to give the title compound as an off-white solid (10 mg, 51%). LCMS purity 100%, m/z 406 [M+H]+.

Provenance & Evidence