2-Pyridinecarboximidamide,3-fluoro-(9CI) synthesis

Yield:757174-04-2 30%

Reaction Conditions:

with N-acetylcystein;ammonium acetate in methanol at 50; for 14 h;

Steps:

4 Synthesis 3-fluoropyridme-2-carboxamidine

3-Fluoro-2-pyridinecarbonitrile (500 mg, 4.1 mmol) and N-acetyl-L-cysteine (75 mg, 0.45 mmol) were dissolved in 4 mL methanol. Ammonium acetate (380 mg, 4.9 mmol) was added and the reaction stirred at 50°C for 14 hours. The solution was evaporated under reduced pressure and purified by flash chromatography. The product was recovered as a tan solid (170 mg, 30%). LCMS (M/Z): 140 (M + H).

References:

WO2015/73797,2015,A1 Location in patent:Page/Page column 37