Reference of 56423-63-3,Some common heterocyclic compound, 56423-63-3, name is 2-Bromopyrazine, molecular formula is C4H3BrN2, 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.
General procedure: A mixture of the respective pyrimidine halide derivative (II) (0.15 mmol), the respective boronic acid derivative (III) (0.18 mmol), and K2003 2M (0.3 mL, 0.6 mmol) in ethanol (3 mL) is purged with argon, tetrakis5 (triphenylphosphine)-palladium (0.0075 mmol) is added, and the RM is heated at 9000 overnight. Alternatively, thereaction can be performed in a microwave apparatus, at 120C for 15- 30 mm. The RM is filtered through a 0.45 um Glass MicroFiber filter, washed with EtOH/MeCN and DMF. The filtrate is purified either by preparative HPLC or FC. Alternatively, it is diluted with water, if needed the pH is adjusted, and extracted with EtOAc (3x). The combined organic extracts are dried (MgSO4) and concentrated under reduced pressure. The residue is purified by preparative HPLC or by FC. The title compound is prepared according to the general procedure A described above, using N-(2-(6-fluoro-4- methoxy-2-methyl-i H-indol-i -yl)ethyl)-6-(4-(4,4,5,5-tetramethyl-i ,3,2-dioxaborolan-2-yl)phenyl)pyrimidin-4-amine and 4-chloro-6-methoxypyrimidine. LC-MS E: tR= 1.10 mm; [M+H]+ =484.88.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Bromopyrazine, its application will become more common.
Reference:
Patent; ACTELION PHARMACEUTICALS LTD; FRETZ, Heinz; LYOTHIER, Isabelle; POTHIER, Julien; RICHARD-BILDSTEIN, Sylvia; SIFFERLEN, Thierry; WYDER PETERS, Lorenza; POZZI, Davide; CORMINBOEUF, Olivier; (306 pag.)WO2017/85198; (2017); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem