Electric Literature of 14399-37-2,Some common heterocyclic compound, 14399-37-2, name is 3,6-Dichloropyrazin-2-amine, molecular formula is C4H3Cl2N3, 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.
To a three-necked round-bottle flask was added Y7d (200 mg, 1.22 mmol, 1 equiv), dioxane (4 mL). The solution was vacuated and purged with nitrogen gas three times. Xantphos (l4mg, 0.024 mmol, 0.02 equiv), PdCh(dppf) (8.9 mg, 0.012 mmol, 0.1 equiv), and DIPEA (0.32 g, 2.44 mmol, 2.0 equiv) were added under nitrogen atmosphere. The solution was heated to 85 C for overnight. The reaction was cooled and evaporated. The residue was purified by columnchromatography (eluent/ethyl acetate/heptane = 1/1) to give Zl7d (259 mg, 0.99 mmol, 81%). ‘H NMR (400 MHz, CDCb) d = 7.83 (s, 1H), 4.88 (bs, 2H), 3.73 (s, 3H), 3.47 (t, J= 9.2 Hz, 2H), 2.79 (t, J= 9.2 Hz, 2H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 3,6-Dichloropyrazin-2-amine, its application will become more common.
Reference:
Patent; NOVARTIS AG; FEI, Zhongbo; LU, Gang; WAN, Yinbo; WANG, Jianhua; WU, Quanbing; ZHANG, Hao; (116 pag.)WO2020/65453; (2020); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem