Water → HCID 178497690, compound

Participants

Reaction Conditions

Reaction Steps

Into a vial was added methyl 3-formylbenzoate (102 mg, 0.6 mmol) and a solution of (R)-(1-(6-amino-5-nitropyridin-2-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone (140 mg, 0.4 mmol) in ethanol (1.5 mL). Sodium dithionate (388 mg, 2.2 mmol) and water (0.5 mL) were added. The vial was sealed and the solution was stirred 110° C. for 18 h. The solution was cooled to room temperature and triethylamine (0.1 mL) was added. The solution was stirred at 100° C. for 18 h. An aliquot of 0.8 mL was removed and concentrated to dryness, and the resulting residue was purified via HPLC to afford the title compound. MS (ESI+) (M+H) 434.2; HPLC retention time 2.25 min (Method A).

Provenance & Evidence