Some common heterocyclic compound, 19745-07-4, name is 2,5-Dichloropyrazine, molecular formula is C4H2Cl2N2, 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. 19745-07-4
A mixture of methyl (R)-3-(3-amino-4-(((1 r,4R)-4-((tert-butyldimethylsilyl)oxy)cyclo hexyl)(isobutyl)amino)phenyl)butanoate (200 mg, 0.42 mmol), 2,5-dichloropyrazine (125 mg, 0.84mmol), Pd2(dba)3 (76 mg, 0.084 mmol), Xantphos (96 mg, 0.168 mmol) and CS2CO3 (273 mg, 0.84 mmol) in toluene (10 mL) was stirred at 100¡ãC under N2 atmosphere overnight. The resulting mixture was partitioned between EtOAc and H20. 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, 0-10percent EtOAc in PE) to afford the title compound (170 mg, 68percent yield). LCMS (ESI) m/z calcd for C31 H49CIN4O3S1: 588.33. Found: 589.62/591 .59 (M/M+2)+.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 19745-07-4, 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