Related Products of 36070-75-4,Some common heterocyclic compound, 36070-75-4, name is 5-Chloropyrazine-2-carbonitrile, molecular formula is C5H2ClN3, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A mixture of methyl (R)-3-(3-amino-4-(isobutyl(tetrahydro-2H-pyran-4-yl)amino)phenyl) butanoate (220 mg, 0.63 mmol), 5-chloropyrazine-2-carbonitrile (177 mg, 1 .27 mmol), Pd2(dba)3 (58 mg, 0.064 mmol), Xantphos (74 mg, 0.13 mmol) and K2C03 (262 mg, 1 .9 mmol) in toluene (10 mL) was stirred at 100C under N2 atmosphere overnight. The resulting mixture was partitioned between EtOAc and H2O. The organic layer was washed with brine, dried over Na2S04, filtered and concentrated to give the crude product which was purified by flash chromatography (silica gel, 0-40% EtOAc in PE) to afford the title compound (70 mg, 25% yield). LCMS (ESI) m/z calcd for C25H33N5O3: 451 .26. Found: 452.46 (M+1)+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 5-Chloropyrazine-2-carbonitrile, its application will become more common.
Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; DE LA ROSA, Martha Alicia; KAZMIERSKI, Wieslaw Mieczyslaw; SAMANO, Vicente; (369 pag.)WO2018/116107; (2018); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem