Formic Acid → Ammonia

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-[6-(3-thienyl)-3-pyridazinyl]-(1S,4S)-(+)-2,5-diazabicyclo-[2.2.1]-heptane (0.21 g, 0.81 mmol), formic acid (0.92 ml, 24.4 mmol) and formaldehyde (0.68 ml, 24.4 mmol) was stirred at 100° C. for 6 hours. The mixture was evaporated. Aqueous sodium hydroxide (30 ml, 1 M) was added followed by extraction with ethyl acetate (3×30 ml). Chromatography on silica gel with dichloromethane, methanol and conc. ammonia (89:10:1) gave the title compound as an oil. Yield 0.15 g, 77%.

Provenance & Evidence