Reference of 76537-18-3, These common heterocyclic compound, 76537-18-3, name is 3-Bromo-5-chloropyrazin-2-amine, its 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.
Intermediate C65-Chloro-3-(2-methylthiazol-5-yI)pyrazi n-2-am i ne A mixture of 2-methyl-5-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)thiazole (1 g, 4.44 mmol), 3-bromo-5-chloropyrazin-2-amine (0.926 g, 4.44 mmol), PdCI2(dppf).CH2CI2 adduct (0.181 g, 0.222 mmol) and 2 M Na2CO3 (6.66 ml) in DME (22.21 ml) under N2 was heatedusing microwave radiation at 120C for 45 mins. The mixture was added to water (100 ml) and extracted with EtOAc (2 x 90 ml). The organic extracts were washed with brine, dried over Mg504 and concentrated under reduced pressure. Purification by chromatography on silica eluting with 0-10% [2.OM NH3 in MeOH] in TBME afforded the title compound as a brown solid;LCMS: Rt 0.87 mins; MS mlz 227.1 [M+H]+; Method 2minLC_v003.
The synthetic route of 76537-18-3 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; NOVARTIS AG; BELLENIE, Benjamin Richard; BLOOMFIELD, Graham Charles; BRUCE, Ian; CULSHAW, Andrew James; HALL, Edward Charles; HOLLINGWORTH, Gregory; NEEF, James; SPENDIFF, Matthew; WATSON, Simon James; (395 pag.)WO2015/162459; (2015); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem