2-Aminopyridine → Tert-butyl 4-(5-amino-6-(pyridin-2-ylcarbamoyl)pyrazin-2-yl)piperazine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

To a mixture of 3-amino-6-(4-tert-butoxycarbonylpiperazin-1-yl)pyrazine-2-carboxylic acid (8.08 g, 24.99 mmol), di(imidazol-1-yl)methanone (4.863 g, 29.99 mmol), DMAP (152.7 mg, 1.250 mmol) and N-ethyl-N-isopropyl-propan-2-amine (8.074 g, 10.88 mL, 62.47 mmol) in DMSO (80.80 mL) was added pyridin-2-amine (4.704 g, 49.98 mmol) and the resulting solution stirred at 110° C. for 20 hours. Water (500 mL) was added and the mixture extracted into EtOAc (3×300 mL), dried and concentrated to give a residue which was triturated with EtOAc and filtered to give the required product as a yellow solid (5.48 g, 55% Yield).

Provenance & Evidence