Cas No.:36070-75-4


Product use:Basic raw materials, organic intermediates, pharmaceutical intermediates

The synthesis process is as follows:

copper(l) iodide; 18-crown-6 ether; N,N-dimethyl-formamide; tetrakis(triphenylphosphine) palladium(0)

Reactants are commercially availlable.
CANCER RESEARCH TECHNOLOGY LIMITED, WO2009/103966, A1, (2009) Synthesis 2-1 -C5-amino-3-chloropyrazine-2-carbonitrile A mixture of 5-bromo-6-chloropyrazin-2-amine (1.00 g, 4.8 mmol), copper (I) iodide (914 mg, 4.8 mmol), 18-crown-6 (95 mg, 0.36 mmol) and tetrak is(triphenylphosphine)palladium (0) (83 mg, 0.072 mmol) was suspended in dry DMF (20 mL) and a stream of nitrogen was passed through it for 5 minutes. Potassium cyanide (312 mg, 4.8 mmol) was added an d the mixture was stirred at room temperature for 30 minutes, then refluxed at 200°C for 3 hours. Th e mixture was cooled and diluted with EtOAc and absorbed onto silica gel (10 g). DMF was removed by evaporation in a Genevac evaporator. The product was purified by flash chromatography, eluting with 1 :1 ethyl acetate-hexane, to yield the title compound as a yellow solid (607 mg, 3.93 mmol, 82perce nt). 1H NMR (d6-DMSO, 400 MHz) delta 8.1 (br s, 2H), 7.87 (s, 1H). LC-MS (1) Rt = 1.20 min; m/z (ESI-) 153 (M-H).